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Restrict the search for
telotristat ethyl
to a specific field?
Status:
Investigational
Source:
NCT00379990: Phase 2 Interventional Completed Arthritis, Rheumatoid
(2006)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
GW 274150 was developed by GlaxoSmithKline as a selective inhibitor of inducible nitric oxide synthase (iNOS; also known as NOS2). Nitric oxide synthase (NOS) is an important chemical involved in the production of NO. Reduction of NOS, and therefore NO, may be an effective technique for the treatment of migraine headache. GW 274150 offered the potential of anti-inflammatory activity in migraine through a novel mechanism of action. The drug has completed phase II of the clinical trials for patients with rheumatoid arthritis and migraine disorders. In addition, GW 274150 was involved in phase I clinical trial for patients with mild asthma. However, all these studied were discontinued.
Status:
Investigational
Source:
NCT00232258: Phase 2 Interventional Completed Ulcerative Colitis
(2005)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Nolpitantium (SR-140333) is a highly selective nonpeptide antagonist of neurokinin-1 (NK1) receptor. Nolpitantium potently, selectively and competitively inhibited substance P binding to NK1 receptors from various animal species, including humans. In vitro, it was a potent antagonist in functional assays for NK1 receptors such as [Sar9, Met(O2)11]substance P-induced endothelium-dependent relaxation of rabbit pulmonary artery and contraction of guinea-pig ileum. Up to 1 mkM, Nolpitantium had no effect in bioassays for NK2 and NK3 receptors. The antagonism exerted by Nolpitantium toward NK1 receptors was apparently non-competitive, with pD2' values between 9.65 and 10.16 in the different assays. Nolpitantium also blocked in vitro [Sar9, Met(O2)11]substance P-induced release of acetylcholine from rat striatum. In vivo, Nolpitantium exerted highly potent antagonism toward [Sar9, Met(O2)11]substance P-induced hypotension in dogs, bronchoconstriction in guinea-pig) and plasma extravasation in rats. Nolpitantium was found to be effective in the modulation of the inflammatory response and airway remodeling in mice. Nolpitantium is reported to cause antagonism of the SP-induced relaxations of human isolated intralobar pulmonary arterial rings. Nolpitantium also blocked the activation of rat thalamic neurons after nociceptive stimulation. Nolpitantium has been shown to reduce the severity of inflammation in trinitrobenzene sulfonic acid-induced colitis in the rat colon. Nolpitantium inhibited mustard oil-induced plasma protein extravasations in the dorsal skin of the rat hind paw. Nolpitantium had been in some phase II clinical trials but further studies were discontinued.
Status:
Investigational
Source:
NCT02653612: Phase 1 Interventional Withdrawn Lung Cancer
(2016)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
EC17 (also known as Folate-FITC) is conjugate consisting of fluorescein isothiocyanate (FITC) conjugated with folate with potential antineoplastic activity. EC17 binds to folate receptors, which are overexpressed on the surfaces of many cancer cells including kidney and ovarian cancer cells. Once bound to the cancer cell through the folate moiety of the conjugate, circulating anti-fluorescein antibodies recognize and bind to the FITC moiety, resulting in antibody-dependent cellular cytotoxicity. EC17 is participating in phase II clinical trials for the treatment of patients with endometrial cancer, endometriosis, lung cancer, renal cell carcinoma. In January 2018, On Target Laboratories initiated a phase III trial to evaluate the safety and efficacy of EC17 injection for patients with ovarian cancer.
Status:
Investigational
Source:
NCT00322673: Phase 2 Interventional Terminated Acute Myeloid Leukemia
(2006)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Status:
Investigational
Source:
NCT04687241: Phase 3 Interventional Active, not recruiting Non-small Cell Lung Cancer
(2021)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Status:
Investigational
Source:
NCT02083380: Phase 2/Phase 3 Interventional Completed Uncomplicated Plasmodium Falciparum Malaria
(2014)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Conditions:
Artefenomel, a novel trioxolane, is a lead candidate for inclusion in a new antimalarial combination, specifically formulated for children.
Artefenomel has been demonstrated curative in as little as one dose.
Status:
Investigational
Source:
NCT00637793: Phase 2 Interventional Completed Xerostomia
(2008)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
NGX267 is a partial muscarinic receptor agonist with functionally specific M1 and M3 receptor activity, developed by Torrey Pines Therapeutics(TPTX) for the treatment of Xerostomia, Alzheimer’s disease and cognitive deficits in schizophrenia. NGX-267 had been in phase II clinical trials for the treatment of Xerostomia, however, all researchers on this drug candidate were discontinued.
Status:
Investigational
Source:
USAN:CINDUNISTAT HYDROCHLORIDE MALEATE [USAN]
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Cindunistat hydrochloride maleate (SD-6010) is an orally-administered, selective, time-dependent and irreversible inhibitor of human iNOS (hiNOS). In vivo studies using the canine anterior cruciate ligament-transection model have demonstrated that cindunistat improves synovial fluid nitrite and nitrotyrosine biomarkers, osteophyte formation and cartilage lesions. Cindunistat has also been shown to improve pain behaviour in rodent models of inflammatory and neuropathic pain. Based on its potential to inhibit NO production and an early clinical development programme, the disease-modifying efficacy and safety profile of cindunistat was studied in a 2-year proof-of-concept clinical trial of patients with knee OA. Cindunistat (50 or 200 mg/day) did not slow the rate of joint space narrowing versus placebo. After 48-weeks, KLG2 patients showed less joint space narrowing; however, the improvement was not sustained at 96-weeks. iNOS inhibition did not slow OA progression in KLG3 patients.
Status:
Class (Stereo):
CHEMICAL (RACEMIC)
Trethinium is tetrahydroisoquinoline derivative. It is an antihypertensive agent.
Status:
Investigational
Source:
NCT01901341: Phase 3 Interventional Terminated Opioid-Induced Constipation
(2013)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Bevenopran (also known as CB-5945), a peripherally acting mu-opioid receptor antagonist that was studied for the treatment of opioid-induced constipation. Due to difficulties with enrollment, phase III of clinical trials were terminated early.
