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VadimezanEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Tumor cells rely on the existence of a specialized vasculature for the oxygen and nutrients that they require in order to grow and survive. Targeting the tumor vasculature as a technique for inhibiting tumor growth was first attempted with angiogenesis inhibitors, a class of drugs that compromise the formation of new blood vessels. More recently a new class of drugs called vascular disrupting agents (VDAs) has been reported. Rather than preventing the formation of new blood vessels, VDAs target endothelial cells and pericytes in the already-established vascular network supporting the tumor. VDAs are designed to induce mass...
Source: Prous Science - Molecule of the Month - October 30, 2009 Category: Chemistry Source Type: info

Influenza (H1N1) 2009 VaccinesEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
(EN:668987, EN:668959, EN:669086, EN:671307, EN:669516, EN:673657, EN:659629) The current pandemic of H1N1 influenza, the first cases of which were detected in Mexico in March 2009, has extended worldwide with astonishing speed, matched only by the speed of response by health authorities and the pharmaceutical industry. On April 27, slightly a month after the first cases were detected, the World Health Organization raised the pandemic alert level to phase 4, indicating confirmed human-to-human transmission of the virus resulting in community-level outbreaks. Just two days later, WHO raised the pandemic alert level to phase...
Source: Prous Science - Molecule of the Month - October 1, 2009 Category: Chemistry Source Type: info

RaxibacumabEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Bacillus anthracis, the organism that causes anthrax infections, was the first bacterium demonstrated to cause a disease. The use of anthrax as a biological weapon dates back to World War I, when the German army is believed to have injected horses, mules and cattle with anthrax toxin. In 1937 Japan initiated a biological warfare program, and the U.S. and U.K. followed suit half a decade later. The United States' biological weapons program was terminated in 1969, and in 1972 the Biological Weapons and Toxins Convention outlawed the development and stockpiling of biological weapons. Since that time, however, this class of we...
Source: Prous Science - Molecule of the Month - September 1, 2009 Category: Chemistry Source Type: info

Xoma-052Email this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Xoma recently presented new results from a phase I clinical trial of XOMA-052, a novel antiinflammatory approach for the treatment of type 2 diabetes. XOMA-052 is a humanized monoclonal antibody (MAb) against interleukin-1beta (IL-1beta), the elevated expression of which has been correlated with damage to insulin-producing beta cells in patients with type 2 diabetes. In this trial, a single intravenous infusion of XOMA-052 (0.01, 0.03 or 0.1 mg/kg) or placebo was administered to individuals with inadequately controlled type 2 diabetes who were subsequently assessed for safety, pharmacokinetics and various diabetes and infl...
Source: Prous Science - Molecule of the Month - August 1, 2009 Category: Chemistry Source Type: info

Tmc-207Email this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
This study validates APT synthase as a target for tuberculosis (Diacon, A.H. et al., New Engl J Med 2009, 360(23): 2397). The second stage of the study, which will evaluate efficacy following 24 weeks of treatment, is currently ongoing and is actively recruiting patients with MDR-TB in South Africa, Peru, Latvia and Russia. Results from the second stage are expected to be available in 2010. In late June, Tibotec and the not-for-profit Global Alliance for TB Drug Development (TB Alliance) announced an agreement to collaborate and share their expertise and resources in order to speed the development of TMC-207, potentially...
Source: Prous Science - Molecule of the Month - June 30, 2009 Category: Chemistry Source Type: info

DenosumabEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Receptor activator of NF-kappaB ligand (RANKL) is a member of the tumor necrosis factor (TNF) family of cytokines that is produced by cells of osteoblastic lineage, and its cellular receptor RANK is present on the surface of hematopoietic osteoclast precursor cells as well as on mature osteoclasts. RANKL is now known to be the common and requisite factor intervening in osteoclast formation in response to all known catalysts. As such, the RANK/RANKL/osteoprotegerin pathway is essential for the process of osteoclastogenesis and modulates the differentiation, activation and survival of osteoclasts, thereby regulating bone res...
Source: Prous Science - Molecule of the Month - May 31, 2009 Category: Chemistry Source Type: info

CatumaxomabEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Malignant ascites is a condition characterized by the abnormal accumulation of fluid in the abdominal cavity. It is caused by an imbalance between plasma flow into and out of the blood and lymphatic vessels, and may develop in patients with cancer —primarily ovarian, endometrial, breast, colorectal, gastric and pancreatic cancers. Generally, the development of malignant ascites can be traced back to the settlement of metastasizing cancer cells in the abdominal cavity. The infiltrating cancer cells disrupt the normal regulation of fluid flow in the peritoneal cavity by simultaneously causing greater plasma inflow as w...
Source: Prous Science - Molecule of the Month - April 30, 2009 Category: Chemistry Source Type: info

AlmorexantEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Orexins (hypocretins) are a class of hypothalamic neuropeptides first described in the late 1990s. They have since been shown to regulate the sleep/wake cycle by maintaining wakefulness, as well as being involved in appetite regulation and energy homeostasis. Orexins A and B bind to two CNS receptors, designated orexin-1 and orexin-2. The cell bodies of orexin-producing neurons are restricted to the dorsal, lateral and posterior hypothalamus and its perifornical nucleus. Axonal projections of these cells are dense in the hypothalamus and extend to the limbic system, thalamus, substantia nigra, raphe, locus coeruleus, ventr...
Source: Prous Science - Molecule of the Month - April 11, 2009 Category: Chemistry Source Type: info

RiociguatEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
(BAY-63-2521) is an oral soluble guanylate cyclase stimulator in phase III clinical development at Bayer Schering Pharma for the treatment of chronic thromboembolic pulmonary hypertension and for the treatment of pulmonary arterial hypertension (PAH). The compound stimulates sGC, which leads to the catalyzing of cyclic guanosine monophosphate (cGMP), resulting in the dilation of blood vessels, lowering of blood pressure and the mediation of tissue-protective effects. In February, Bayer Schering Pharma initiated two phase III clinical trials of riociguat: CHEST-1 (chronic thromboembolic pulmonary hypertension sGC stimulat...
Source: Prous Science - Molecule of the Month - March 2, 2009 Category: Chemistry Source Type: info

TelcagepantEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
In this study, 1,380 patients diagnosed with moderate to severe migraine according to International Headache Society (IHS) criteria were treated with telcagepant (150 or 300 mg), zolmitriptan (5 mg) or placebo. Five co-primary endpoints were evaluated at 2 hours postdosing: pain freedom, pain relief, absence of photophobia, absence of phonophobia and absence of nausea. Telcagepant was significantly more effective than placebo in terms of all five endpoints. Furthermore, while the efficacy of the CGRP antagonist was comparable to that of the zolmitriptan, telcagepant was associated with fewer adverse events (Ho, T.W. et al....
Source: Prous Science - Molecule of the Month - February 2, 2009 Category: Chemistry Source Type: info

TelavancinEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
The emergence of multidrug-resistant Gram-positive pathogens has created a need for newer antibacterial agents with improved efficacy. Researchers have focused on modifying the antibiotic vancomycin and other glycopeptides by adding hydrophobic substituents in order to improve activity, absorption, distribution, metabolism and excretion. Telavancin is one such novel antibiotic that was found to have multiple mechanisms of action, including inhibition of bacterial cell wall formation and disruption of cell membrane integrity. The agent showed potent activity in vitro and in vivo against methicillin-resistant Staphylococcus ...
Source: Prous Science - Molecule of the Month - January 3, 2009 Category: Chemistry Source Type: info

AgomelatineEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Tricyclic antidepressants, while effective in treating mild to severe forms of depression, are associated with an extensive tolerability profile, making them a nonviable option to many patients. The newer selective serotonin reuptake inhibitors (SSRIs) are better tolerated when compared with their tricyclic predecessors, and have recently become the most widely used antidepressant agents. However, problems with specific side effects (particularly affecting sexual function) have compromised treatment compliance in some patients. There is also evidence to suggest that while SSRIs are effective in mild to moderate forms of de...
Source: Prous Science - Molecule of the Month - November 29, 2008 Category: Chemistry Source Type: info

DirucotideEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Multiple sclerosis (MS) is one of the most common diseases of the central nervous system, affecting more than 2,500,000 people around the world. MS is the result of damage to myelin, a protective sheath surrounding nerve fibres of the central nervous system. When myelin is damaged, this interferes with messages between the brain and other parts of the body. Altered peptide ligands (APLs) are analogues of peptide determinants with one or more substitutions at the amino acid positions required for contact with the T cell receptor. APLs can act as either partial agonists or antagonists of the T cell receptor in question. In t...
Source: Prous Science - Molecule of the Month - October 31, 2008 Category: Chemistry Source Type: info

TecovirimatEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
In 1980, the World Health Organization declared that variola virus, the etiologic agent of smallpox, had been eradicated on a global level. However, two decades later concerns remain that this infectious agent, which has an alarmingly high morbidity and mortality rate, could be used as an agent of biological warfare. In recent years investigation into potential new vaccines and antiviral drugs for the treatment and prevention of smallpox virus infection has gained renewed strength, driven in part by support from the U.S. FDA and Centers for Disease Control and Prevention (CDC). Tecovirimat (ST-246), an inhibitor of ortho...
Source: Prous Science - Molecule of the Month - October 1, 2008 Category: Chemistry Source Type: info

MipomersenEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
(ISIS-301012) is a 20-mer antisense chimeric phosphorothiate oligonucleotide that selectively targets apolipoprotein B (apoB), a protein critical to the synthesis and transport of LDL and VLDL cholesterol, both involved in the development of heart disease. It is in phase III clinical trials at Isis Pharmaceuticals for the subcutaneous treatment of familial hypercholesterolemia. The compound is also in phase II clinical development for the treatment of hypercholesterolemia, and in phase II in combination with simvastatin for the treatment of atherosclerosis in patients with high cholesterol. In June 2006, mipomersen receiv...
Source: Prous Science - Molecule of the Month - September 2, 2008 Category: Chemistry Source Type: info

Icatibant AcetateEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Hereditary angioedema (HAE) is an uncommon hereditary disorder that can cause sudden and severe attacks of nonpitting edema that may affect any external or mucosal surface including the face, arms, legs, hands, feet, genitalia, digestive track and airway. Although it is uncomfortable and cosmetically unacceptable, it is rarely dangerous. Severe urticaria or angioedema, however, may sometimes cause swelling of mucous membranes of the respiratory or gastrointestinal tracts, resulting in anaphylaxis or asphyxiation. The pathogenesis of HAE is due to a mutation in the gene encoding for the plasma protein C1 inhibitor. Treatmen...
Source: Prous Science - Molecule of the Month - August 1, 2008 Category: Chemistry Source Type: info

SemagacestatEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Deposition of amyloid beta (Abeta) peptide into plaques is one of the two hallmark features of Alzheimer's disease. These plaques, typically concentrated in the spaces between nerve cells in the brain parenchyma and cerebral blood vessel walls, are thought to impede nerve cell function and promote neuronal degeneration in Alzheimer's disease brains. According to current thinking, AD etiology is explained by the amyloid cascade hypothesis, whereby overproduction of Abeta protein, or alternatively the failure to clear this protein, leads to the accumulation of amyloid deposits and contributes to the formation of neurofibrill...
Source: Prous Science - Molecule of the Month - June 30, 2008 Category: Chemistry Source Type: info

EltrombopagEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Thrombopoietin (TPO) is a glycoprotein hormone produced primarily by the liver that activates megakaryocytes in the bone marrow, causing them to differentiate and fragment into platelets. Under normal circumstances, the bloodstream platelet counts range from 150,000 to 400,000/mcl. However, under conditions of thrombocytopenia, platelet counts may drop below 50,000/mcl. Under these circumstances, patients are predisposed to bleeding, particularly at mucous membranes, and in some cases bleeding may become severe enough to require treatment. Thrombocytopenia is commonly associated with cancer chemotherapy and a number of oth...
Source: Prous Science - Molecule of the Month - May 30, 2008 Category: Chemistry Source Type: info

OdanacatibEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Cathepsin K is a cysteine protease that is selectively and highly expressed by osteoclasts and secreted into the extracellular compartment, where it cleaves important bone matrix proteins, acting as the principal effector of bone degradation during the process of bone resorption. Activated cathepsin K degrades various bone matrix components including type I collagen, osteopontin and osteonectin. It is an attractive target for modulation in osteoporosis and other disorders caused by excessive bone resorption, because while it is expressed at high levels in bone, it is present at extremely low levels in the heart, liver, lun...
Source: Prous Science - Molecule of the Month - May 2, 2008 Category: Chemistry Source Type: info

RilonaceptEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Cryopyrin-Associated Periodic Syndromes (CAPS) are a recently identified group of rare, inherited auto-inflammatory disorders characterized by life-long, recurrent symptoms of rash, fever/chills, joint pain, eye redness/pain and fatigue. Intermittent, disruptive exacerbations or flares can be triggered at any time by exposure to cooling temperatures, stress, exercise or other unknown stimuli. Three related conditions fall under the classification of CAPS: Familial Cold Auto-inflammatory Syndrome (FCAS), Muckle-Wells Syndrome (MWS) and Neonatal-Onset Multisystem Inflammatory Disease (NOMID). The incidence of CAPS has been r...
Source: Prous Science - Molecule of the Month - March 31, 2008 Category: Chemistry Source Type: info

UstekinumabEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
In this study, patients responding to ustekinumab at week 40 were randomized to either continue treatment or switch to placebo. At week 52, 87% and 91% of patients receiving ustekinumab 45 and 90 mg, respectively, maintained a PASI 75 response, compared to 64% and 62% of placebo-treated patients. Long-term maintenance therapy was generally well tolerated, with 46% and 49% of patients in the 45 and 90 mg dose groups, respectively, experiencing at least one adverse event after randomization at week 40, compared to 56% and 48% of patients switched to placebo (Gordon, K.B. et al., J Am Acad Derm...
Source: Prous Science - Molecule of the Month - February 29, 2008 Category: Chemistry Source Type: info

MaravirocEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Despite the availability of several approved drugs for the treatment of human immunodeficiency virus (HIV) infection, the limited effectiveness of current antiretroviral regimens, mainly due to the emergence of resistance, makes the development of new agents necessary. Several novel compounds are being added to existing classes, but the discovery and development of newer classes of antiretroviral drugs, such as HIV entry inhibitors, represents a significant advance in the treatment of AIDS and HIV. HIV enters the host cell by a sequential process that requires engagement with CD4 followed by binding to a coreceptor: eithe...
Source: Prous Science - Molecule of the Month - February 1, 2008 Category: Chemistry Source Type: info

Obatoclax mesylateEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
(GX15-070) is a small-molecule indole bipyrrole drug compound and pan-Bcl-2 family inhibitor being developed at Gemin X Biotechnologies for the treatment of cancer. Recently published studies have confirmed the mechanism of action of the compound, demonstrating that it specifically disrupts the survival of cancer cells as a result of inhibiting the Bcl-2 pro-survival protein Mcl-1. Elevated expression of members of the Bcl-2 pro-survival family of proteins can confer resistance to apoptosis in cancer cells, and obatoclax overcomes Bcl-2 pro-survival proteins' resistance to the pro-apoptotic proteins BAX and BAK. The anti-...
Source: Prous Science - Molecule of the Month - December 31, 2007 Category: Chemistry Source Type: info

ElesclomolEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Synta Pharmaceuticals' elesclomol (STA-4783), a first-in-class small-molecule oxidative stress inducer, has been selected as the Molecule of the Month. Elesclomol induces an oxidative stress response in cancer cells by inducing heat shock protein 70 (Hsp70), thereby inducing apoptosis and enhancing the activity of certain anticancer agents such as paclitaxel. In October, Synta signed a global collaboration agreement with GlaxoSmithKline for the joint development and commercialization of elesclomol. Under the terms of the agreement, the companies will share responsibility for development and commercialization of elesclomol ...
Source: Prous Science - Molecule of the Month - November 30, 2007 Category: Chemistry Source Type: info

DapagliflozinEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Sodium-dependent glucose transport proteins (SGLTs) play a key role in maintaining glucose homeostasis in the human body. SGLTs are found in the intestine (SGLT1) and the kidney (SGLT1 and SGLT2). Renal SGLT reabsorbs glucose from the renal filtrate, thus preventing loss of glucose in urine. Renal SGLTs are found in the pars convoluta of the nephron's proximal tubule. SGLTs use the energy from a positive sodium gradient to transport glucose across the membrane. SGLT2 has a 1:1 ratio of sodium-glucose transport. SGLT1 works similarly but has a 2:1 ratio of sodium-glucose transport. SGLT2 accounts for 98% of renal glucos...
Source: Prous Science - Molecule of the Month - October 31, 2007 Category: Chemistry Source Type: info

Sugammadex sodiumEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
, a reversal agent used during general anesthesia, is the first selective relaxant binding agent (SRBA), a drug-specific cyclodextrin that is specifically designed to reverse the effects of the muscle relaxant rocuronium bromide (Esmeron®/Zemuron®) when the latter is used as a component of general anesthesia during surgical procedures. Current reversal agents can only be administered when muscle relaxation is starting to wear off naturally; however, sugammadex can achieve reversal following rocuronium bromide administration within three minutes, regardless of the depth of block. Furthermore, in studies to date, sug...
Source: Prous Science - Molecule of the Month - October 1, 2007 Category: Chemistry Source Type: info

APC-366 (Arris; Bayer) Marimastat (British Biotech)Email this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Marimastat is an orally active, second-generation matrix metalloproteinase inhibitor (MMPI) from British Biotech that is currently undergoing extensive phase II evaluation in several countries, including the U.S. and the U.K., for the treatment of patients with advanced solid tumors, such as colorectal, ovarian, pancreatic and prostatic tumors. Unlike conventional anticancer agents, MMPIs are not cytotoxic, but rather act to prevent the spread or progression of cancers. They are thus expected to have little effect on normal tissue, and are intended for use as maintenance therapy following chemotherapy or surgery, or for po...
Source: Prous Science - Molecule of the Month - September 10, 2007 Category: Chemistry Source Type: info

Atorvastatin (Warner-Lambert), N-0923 transdermal patch (Discovery Therapeutics) and NN-42-1007 (Novo NordiskEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Warner-Lambert is filing regulatory submissions for its HMG-CoA reductase inhibitor, atorvastatin, this month in the United States, France, the United Kingdom, Australia, New Zealand, Switzerland and South Africa, and filings are expected soon in Germany and Canada. Atorvastatin reportedly represents an advance over existing statin compounds as a lipid regulator. It has been shown particularly effective at lowering total cholesterol and LDL-cholesterol, where reductions on the order of 60% have been demonstrated. The first clinical data on the pharmacokinetics and safety of Discovery Therapeutics' N-0923 transdermal pa...
Source: Prous Science - Molecule of the Month - September 10, 2007 Category: Chemistry Source Type: info

Cgp-52608Email this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Ciba has identified a lead compound, CGP-52608, from a series of thiazolidinediones that are highly effective in suppressing chronic inflammation and joint destruction in the rat adjuvant arthritis model. CGP-52608 was found to specifically activate the retinoid Z receptor (RZR)/retinoic acid receptor-related orphan receptor alpha (ROR alpha) at low concentrations, and structure-activity studies with analogues demonstrated a marked correlation between RZR/ROR alpha activation and antiarthritic activity. This receptor is a member of the superfamily of inducible transcription factors, and researchers at Ciba recently...
Source: Prous Science - Molecule of the Month - September 10, 2007 Category: Chemistry Source Type: info

TazaroteneEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
(AGN-190168; Allergan) is the first of a new generation of receptor-selective retinoids specifically designed for the topical treatment of mild to moderate plaque psoriasis. Data from a large-scale, controlled clinical trial have demonstrated that tazarotene in a topical gel formulation is safe and efficacious, and that it continues to show therapeutic effects 12 weeks posttreatment (Drake, L. et al. Clin Dermatol 2000 (May 28-31, Vancouver) 1996, Abst. 352; see also abstracts 351 and 353). (Source: Prous Science - Molecule of the Month)
Source: Prous Science - Molecule of the Month - September 10, 2007 Category: Chemistry Source Type: info

PramlintideEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
, an analog of the natural human hormone amylin, is in development by Amylin and Johnson & Johnson for improving glucose control in patients with type 1 or 2 diabetes who use insulin, thereby reducing the risk of diabetic complications. Results from a recent phase II trial in patients with type 2 diabetes who self-administered the drug for one month demonstrated its ability to significantly reduce blood glucose concentrations without causing hypoglycemia, and reaffirmed its good short-term safety. Six phase III trials are in progress in the U.S. and Europe (Amylin News Release). (Source: Prous Science - Molecule of the Month)
Source: Prous Science - Molecule of the Month - September 10, 2007 Category: Chemistry Source Type: info

BuckminsterfullereneEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
The Royal Swedish Academy of Sciences has awarded the 1996 Nobel Prize in Chemistry jointly to Professor Robert F. Curl, Jr. and Professor Richard E. Smalley, both of Rice University (Houston, TX, U.S.A.) and Professor Sir Harold W. Kroto of the University of Sussex (Brighton, U.K.), for their discovery of the fullerenes. These compounds, new forms of the element carbon, were discovered by the trio in 1985 and first published in the scientific journal Nature in November of the same year. Fullerenes are formed when vaporized carbon condenses in an atmosphere of inert gas. The gaseous carbon is obtained by methods such as di...
Source: Prous Science - Molecule of the Month - September 10, 2007 Category: Chemistry Source Type: info

Clopidogrel hydrogensulfateEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
is a new thienopyridine antiplatelet agent discovered by Sanofi that prevents blood clot formation inside an atherosclerotic artery by inhibiting platelet activation and aggregation. Sanofi recently announced the results of the large, international CAPRIE (Clopidogrel versus Aspirin in Patients at Risk of Ischemic Events) trial at the 69th Scientific Sessions of the American Heart Association, showing a significant reduction in such events compared to aspirin, as well as good safety. The CAPRIE study demonstrated that treatment with clopidogrel provided an overall relative risk reduction for ischemic stroke, myocardial in...
Source: Prous Science - Molecule of the Month - September 10, 2007 Category: Chemistry Source Type: info

Lgd-1069Email this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Interim results from a phase I/II clinical trial assessing Ligand Pharmaceuticals' TargretinTM (LGD-1069) topical gel formulation in 30 patients with cutaneous T cell lymphoma (CTCL) were reported at the American Society of Hematology annual meeting in Orlando, Florida, in early December 1996. The trial was designed to assess the safety and efficacy of escalating doses (beginning as 0.1% gel q.d., escalated every two weeks as tolerated to 0.1% b.i.d., 0.5% q.d., 0.5% b.i.d., 1.0% q.d. and 1.0% b.i.d.) of the product in patients with stage I/IIa CTCL. A retinoid X receptor (RXR) receptor-selective retinoid, Targretin was ge...
Source: Prous Science - Molecule of the Month - September 10, 2007 Category: Chemistry Source Type: info

ZileutonEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
is a selective, orally active inhibitor of 5- lipoxygenase (5-LO) from Abbott, proven to exert antiinflammatory and antiallergic effects in animal models and humans. The FDA cleared zileuton (Zyflo[TM]) for the prevention and chronic treatment of asthma in patients at least 12 years of age in December, and Abbott launched it on January 28th (Abbott News Release). (Source: Prous Science - Molecule of the Month)
Source: Prous Science - Molecule of the Month - September 10, 2007 Category: Chemistry Source Type: info

Donepezil hydrochlorideEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
(Aricept[TM]) is a reversible acetylcholinesterase inhibitor discovered by Eisai, available as of this week in the U.S. for the treatment of mild to moderate symptoms of Alzheimer's disease. It has also been submitted for approval in the U.K. and will be comarketed/copromoted in these two countries by Eisai and Pfizer. Pfizer also holds codevelopment rights in Japan and certain other European countries, and exclusive rights in Canada and Australia. Bracco has been granted copromotion rights to the drug for Italy. (Source: Prous Science - Molecule of the Month)
Source: Prous Science - Molecule of the Month - September 10, 2007 Category: Chemistry Source Type: info

Gs-4104Email this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Researchers at Gilead Sciences, the University of California, Berkeley, and the Australian National University have discovered and developed a novel class of carbocyclic compounds for the treatment and prevention of influenza (flu) --the neuraminidase inhibitors-- which block an enzyme necessary for the replication of the virus. The lead compound, GS-4104, exhibits potent, broad-spectrum activity against multiple strains of influenza A and B, is orally active and appears to be devoid of side effects. Gilead and Roche are collaborating on the development and worldwide commercialization of GS-4104 for both the prevention and...
Source: Prous Science - Molecule of the Month - September 10, 2007 Category: Chemistry Source Type: info

LobucavirEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
(BMS-180194) was identified by Bristol-Myers Squibb as the active enantiomer of BHCG (SQ-33054), a cyclobutane nucleoside analogue with antiviral activity against herpesviruses and HIV. Lobucavir has a broad spectrum of activity against herpesviruses, including aciclovir-resistant herpes simplex virus (HSV) and ganciclovir-resistant cytomegalovirus (CMV), and hepatitis B. It has good oral bioavailability and is also effective when given topically. Results from clinical studies have demonstrated its safety and efficacy against CMV infection in HIV-infected patients after oral administration. (Source: Prous Science - Molecule of the Month)
Source: Prous Science - Molecule of the Month - September 10, 2007 Category: Chemistry Source Type: info

Synthesis of epothilones opens up new avenue of anticancer researchEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
The epothilones are a new class of natural cytotoxic agents originally isolated from a cultured strain of the myxobacterium Sorangium cellulosum. These compounds work in the same way as paclitaxel (Taxol) to inhibit cancer cell proliferation, promoting microtubule assembly and stabilization, but results from in vitro studies indicate that they are also active against paclitaxel- resistant cancer cell lines. Although several syntheses of epothilone A and epothilone B have been reported, the first solid-phase synthesis of epothilone A and the total synthesis of epothilone B, as well as the synthesis of epothilone analog...
Source: Prous Science - Molecule of the Month - September 10, 2007 Category: Chemistry Source Type: info

Raloxifene hydrochlorideEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
At the 4th International Symposium on Osteoporosis Research Advances and Clinical Applications, held in Washington, D.C., U.S.A., June 4-7, 1997, researchers from Eli Lilly and Co. presented encouraging results from a phase III trial of raloxifene hydrochloride (LY-139481), a selective estrogen receptor modulator (SERM), as an alternative to hormone replacement therapy in the prevention of postmenopausal health risks, including osteoporosis. The compound increased bone mineral density, an indicator of risk for fracture, by 2-3% compared with placebo at all skeletal sites measured (hip, spine and total body). The increases ...
Source: Prous Science - Molecule of the Month - September 10, 2007 Category: Chemistry Source Type: info

Vx-710Email this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
VX-710 is a new chemosensitizing agent under development by Vertex and its Canadian partner BioChem Therapeutic that is designed to restore the tumor-killing activity of chemotherapeutic agents in patients with cancer complicated by multidrug resistance (MDR). The compound reverses MDR by blocking both the P-glycoprotein (MDR1) and multidrug resistance-associated protein (MRP) mechanisms. In a phase I/II trial in patients with solid tumors, treatment with VX-710 and paclitaxel was well tolerated and the coadministration of VX-710 resulted in a significant paclitaxel-sparing effect, allowing the use of significantly...
Source: Prous Science - Molecule of the Month - September 10, 2007 Category: Chemistry Source Type: info

TNK-tPEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
A is a bioengineered drug designed to be administered as a single intravenous injection over 5-10 seconds, dissolving clots that cause heart attacks without interfering with other clotting factors. Results from two new phase II studies on TNK-tPA were presented at the 19th Congress of the European Society of Cardiology, held in Stockholm, Sweden, August 24-28, 1997. TNK-tPA was found to have a comparable efficacy and safety profile to the 90-minute infusion of tissue plasminogen activator (tPA), the current standard treatment for heart attacks. The two phase II studies were conducted in parallel to evaluate the efficacy ...
Source: Prous Science - Molecule of the Month - September 10, 2007 Category: Chemistry Source Type: info

EfavirenzEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
(DMP-266, Sustiva[TM]) is a non-nucleoside reverse transcriptase inhibitor (NNRTI) from DuPont Merck which is undergoing extensive evaluation in combination with other antiretroviral agents and is currently in phase III trials for the treatment of HIV infection and AIDS. In phase II trials, significant suppression of HIV RNA was observed after monotherapy, and combination therapy with indinavir sulfate (Crixivan; Merck & Co.) reduced viral load to below the level of detection in a high percentage of patients and increased CD4 cell counts. Efavirenz has been detected in cerebrospinal fluid, is active against certain mu...
Source: Prous Science - Molecule of the Month - September 10, 2007 Category: Chemistry Source Type: info

Hmr-3647Email this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
HMR-3647 (RU-66647) is a new ketolide antibacterial agent in development by Hoechst Marion Roussel which has undergone extensive evaluation in vitro and in vivo. A number of in vitro studies were presented recently at the 37th Interscience Conference on Antimicrobial Agents and Chemotherapy in Toronto, demonstrating its potent and broad-spectrum activity. HMR-3647 displays antipneumococcal activity (including penicillin-resistant strains), excellent activity against respiratory pathogens, activity against vancomycin-resistant enterococci, as well as potential in the treatment of sexually transmitted and pelvic inflammatory...
Source: Prous Science - Molecule of the Month - September 10, 2007 Category: Chemistry Source Type: info

RepaglinideEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
A new oral treatment for type II diabetes is being fast-tracked by the FDA and was recently recommended for approval for the treatment of type II diabetics not satisfactorily controlled by diet and exercise alone. Repaglinide (Prandin[TM]; NovoNorm[R] outside the U.S.) is the first in a new class of short- and fast-acting insulin release-promoting agents which is designed to regulate postprandial glucose loads. The nonsulfonylurea compound was codeveloped by Novo Nordisk and Boehringer Ingelheim, and the former holds worldwide marketing rights. Novo Nordisk has also filed for approval in the E.U., Norway, Switzerland and C...
Source: Prous Science - Molecule of the Month - September 10, 2007 Category: Chemistry Source Type: info

BecaplerminEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
The FDA recently approved Regranex® Gel (0.01%) as the first biologic for the treatment of diabetic foot ulcers. The active ingredient in Regranex® is becaplermin, a genetically engineered platelet-derived growth factor (rhPDGF-BB) developed and manufactured by Chiron. It mimics the effects of natural PDGF, stimulating the migration of cells to the ulcer site and thereby promoting the growth of new tissue. The gel will be marketed by Ortho-McNeil. (Source: Prous Science - Molecule of the Month)
Source: Prous Science - Molecule of the Month - September 10, 2007 Category: Chemistry Source Type: info

Ro-61-1790Email this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Endothelin (ET) has been implicated in a number of disorders, such as congestive heart failure and cerebral vasospasm following subarachnoid hemorrhage (SAH), and a potent ETA receptor antagonist suitable for parenteral administration appears to be of special interest in cerebral vasospasm. Unfortunately, endothelin antagonists have not yet fulfulled their promise as potential therapeutic agents for a variety of reasons, including low potency and low water solubility. Roche's Ro-61-1790, a follow-up compound to bosentan, the first ET antagonist to be tested in the clinic, belongs to a new generation of trifunctiona...
Source: Prous Science - Molecule of the Month - September 10, 2007 Category: Chemistry Source Type: info

Living Human Skin Equivalent Apligraf TMEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
February's 'Molecule of the Month' is not a molecule at all, but a manufactured living human skin equivalent developed by Organogenesis. Apligraf TM features both an epidermis and a dermis: the upper layer is comprised of living human epidermal cells (keratinocytes) and the lower layer of living human dermal cells (fibroblasts) in an organized dermal matrix. The skin equivalent thus takes as a graft and directly contributes to the wound-healing process by interacting with the wound bed. Apligraf TM is organized using Organogenesis' proprietary organotypic culturing technology which enables the cells to reproduce ...
Source: Prous Science - Molecule of the Month - September 10, 2007 Category: Chemistry Source Type: info

TNFR:Fc (EnbrelTM)Email this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
A novel genetically engineered product developed by Immunex in collaboration with the Wyeth-Ayerst division of American Home Products has recently been designated a "fast track product" for the treatment of advanced rheumatoid arthritis by the FDA, meaning that the agency will help expedite the development and review of the product. EnbrelTM (also referred to as TNF receptor, TNFR and TNFR:Fc) binds to and inhibits the activity of the proinflammatory cytokine TNF, thereby blocking the inflammatory response associated with rheumatoid arthritis. Clinical trials in patients with active rheumatoid arthritis, including those fa...
Source: Prous Science - Molecule of the Month - September 10, 2007 Category: Chemistry Source Type: info

ParicalcitolEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
A new synthetic analogue of 1,25-dihydroxyvitamin D3 that retains the suppressive effect on parathyroid hormone (PTH) but shows minimal effects on calcium and phosphate metabolism was recently approved by the FDA for use in the prevention and treatment of secondary hyperparathyroidism associated with chronic renal failure. Abbott's paricalcitol is the first vitamin D analogue to be approved for this indication. The company plans to introduce the product as Zemplar(TM) by the end of May. (Source: Prous Science - Molecule of the Month)
Source: Prous Science - Molecule of the Month - September 10, 2007 Category: Chemistry Source Type: info