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Restrict the search for
chlorphenesin carbamate
to a specific field?
Class (Stereo):
CHEMICAL (ACHIRAL)
Bamnidazole was developed as an antiprotozoal agent against Tryhomonas, however, has never been marketed.
Class (Stereo):
CHEMICAL (ABSOLUTE)
Alestramustine is the l-alanine ester form of estramustine, a combination of the nitrogen mustard normustine coupled via a carbamate to estradiol, with antineoplastic activity. Upon conversion of alestramustine to estramustine, estramustine binds to microtubule-associated proteins (MAPs) and beta tubulin, thereby interfering with microtubule dynamics and leading to microtubule disassembly and cell cyle arrest. Due to the estrogen moiety, this agent is able to selectively bind to and be taken up by estrogen receptor-positive cells.
Class (Stereo):
CHEMICAL (ACHIRAL)
Capravirine (S-1153, AG1549) is a 1,2,4,5-tetrasubstituted imidazole derivative patented by pharmaceutical company Shionogi as specific inhibitors of HIV-1 reverse transcriptase. However, safety and efficacy studies showed that Capravirine had no specific advantages over currently used NNRTIs. Consequently, clinical trials were discontinued after phase IIb.
Status:
Investigational
Class (Stereo):
CHEMICAL (ABSOLUTE)
Brecanavir (previously known as VX-385), a HIV aspartyl protease inhibitor was developed for the treatment of HIV. The inhibition of HIV viral proteinase enzyme prevents cleavage of the gag-pol polyprotein, resulting in noninfectious, immature viral particles. Brecanavir reached Phase II development. However, GlaxoSmithKline announced to discontinue development brecanavir. Because of the inability to develop a viable oral dosage formulation capable of delivering the desired brecanavir levels in patients with multi-drug resistant HIV.
Status:
Investigational
Source:
NCT01086267: Phase 1/Phase 2 Interventional Completed Colorectal Cancer
(2010)
Source URL:
Class (Stereo):
CHEMICAL (RACEMIC)
BMS-908662 (previously known as XL281) is a small molecule Raf kinase inhibitor that lies immediately downstream of RAS and are key components of the RAS/RAF/MEK/ERK kinase-signaling pathway. Bristol-Myers Squibb has received an exclusive worldwide license to develop and commercialize antineoplastic agent XL281. BMS-908662 participated in phase I development for the treatment of patients with melanoma and in combination with cetuximab for patients with colorectal cancer. However, further, development has been discontinued.
Class (Stereo):
CHEMICAL (RACEMIC)
Targets:
Conditions:
Lemildipine is a 1,4-dihydropyridine calcium channel blocker which is under phase III development by Banyu (Merck and Co), in Japan, for its potential to treat hypertension and cerebrovascular ischemia. In one study, involving five patients with essential hypertension accompanied by cerebrovascular disorder, lemildipine, administered orally at doses of 5 to 20 mg/day, significantly lowered blood pressure and increased cerebral blood flow. Another study in 31 patients with essential hypertension demonstrated that lemildipine has significant pressure lowering effects without affecting serum lipids. Worldwide rights to market the drug have been assigned to Kowa in Japan.
Class (Stereo):
CHEMICAL (ACHIRAL)
Entinostat (MS-275) is an orally active, highly selective, small-molecule histone deacetylase inhibitor (HDACi) derived from benzamide. Entinostat preferentially inhibited HDAC1 versus HDAC3 and had no inhibitory activity toward HDAC8. The time to maximum plasma concentration (tmax) of entinostat ranged from 0.5 to 60h (median of 2h). Elimination of the drug was bi-exponential, with a terminal half-life of 30-80h. Entinostat is a well-tolerated that demonstrates promising therapeutic potential in both solid and hematologic malignancies. Its efficacy does not appear directly dose-related, and as such, more relevant biomarkers are needed to adequately assess its activity.
Status:
Investigational
Source:
INN:disermolide [INN]
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Disermolide (discodermolide) is the immunosuppressant and antineoplastic agent. The marine natural product discodermolide was first isolated in 1990 from the deep-water Caribbean sponge Discodermia dissoluta. It attacks cancer cells in a similar way to the successful cancer drug Taxol that has become the best-selling anticancer drug in history. Discodermolide is a microtubule-stabilizing agent with potential for the treatment of taxol-refractory malignancies. Discodermolide is a drug that functions as an immunosuppressant and induces G2/M phase cell-cycle arrest in lymphoid and non-lymphoid cells. The cytotoxicity of discodermolide cause cell-cycle arrest by mitosis and an important alteration at the level of microtubules. Discodermolide is a potent inducer of accelerated senescence. At present, Phase I trials with discodermolide has been discontinued as a consequence of unsafe efficacy and toxicity results.
Status:
Investigational
Source:
NCT01167244: Phase 2 Interventional Completed Non-Small-Cell Lung Carcinoma
(2010)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Conditions:
BMS-690514 is a potent, reversible oral inhibitor of epidermal growth factor receptor (EGFR/HER-1), HER-2 and -4, and vascular endothelial growth factor receptors (VEGFRs)-1 to -3 offering targeted inhibition of tumour growth and vascularisation in a single agent. Bristol-Myers Squibb was developing BMS 690514, as an oral treatment for cancer. BMS-690514 had being in phase II for the treatment of breast cancer; non-small cell lung cancer, but later these studies were discontinued.
Class (Stereo):
CHEMICAL (ACHIRAL)
FLOSATIDIL is an antihypertensive drug discontinued in Phase II for angina pectoris.
