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Restrict the search for
telotristat ethyl
to a specific field?
Status:
Investigational
Source:
NCT02755311: Phase 3 Interventional Unknown status Hepatocellular Carcinoma
(2014)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Conditions:
10-Hydroxycamptothecin (10-HCPT), an indole alkaloid isolated from a Chinese tree, Camptotheca acuminate, inhibits the activity of topoisomerase I and has a broad spectrum of anticancer activity in vitro and in vivo. However, its use has been limited due to its water-insolubility and toxicity with i.v. administration. Prolonged elimination of 10-HCPT in vivo may have a significant impact on its therapeutic effects. 10-HCPT is metabolized to its carboxylate form and glucuronides.It was investigated that relatively low dose of 10-HCPT is able to inhibit the growth of colon cancer, facilitating the development of a new protocol of human trials with this anticancer drug.
Status:
Investigational
Source:
NCT02889302: Phase 3 Interventional Completed Spinocerebellar Degeneration
(2016)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Ravatirelin is a thiazolyl-alanine derivative patented by Japanese pharmaceutical company Shionogi & Co., Ltd. as a thyrotropin-releasing compound with improved central nerve activating effects such as sustained acetylcholine-releasing effect, and spontaneous motility increasing effect. Rovatirelin binds to the human thyrotropin-releasing hormone receptor with nanomolar affinity and increases the spontaneous firing of action potentials in the acutely isolated noradrenergic neurons of rat locus coeruleus. In in vivo studies, oral administration of Ravatirelin increased both c-Fos expression in the LC and extracellular levels of noradrenaline in the medial prefrontal cortex of rats. Furthermore, Ravatirelin increased locomotor activity. The increase in noradrenaline level and locomotor activity by Ravatirelin was more potent and longer acting than those by taltirelin. In phase I studies in healthy adult males, Ravatirelin exhibited linear pharmacokinetics in a single-ascending dose (0.1 to 10 mg) and a benign safety profile supportive of once-daily oral administration. From results of Phase II and III studies to evaluate the efficacy and safety of Ravatirelin in spinocerebellar degeneration patients, a daily dose of 1.6 to 3.2 mg of Ravatirelin has been considered to be dosage level intended for clinical use as once-daily oral administration.
Status:
Investigational
Source:
NCT01458288: Phase 2 Interventional Completed Multiple Myeloma
(2012)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Burixafor is an orally bioavailable inhibitor of CXC chemokine receptor 4 (CXCR4) with receptor binding and hematopoietic stem cell-mobilization activities. Burixafor binds to the chemokine receptor CXCR4, thereby preventing the binding of stromal derived factor-1 (SDF-1 or CXCL12) to the CXCR4 receptor and subsequent receptor activation; this may induce the mobilization of hematopoietic stem and progenitor cells from the bone marrow into the blood. CXC motif chemokine receptor 4 (CXCR4) blockade is pursued as an alternative to mesenchymal stem cell treatment after heart transplantation. The augmentation of conventional mycophenolate mofetil plus corticosteroids with a CXCR4 antagonist is potentially effective in improving outcomes after heart transplantation in humans
Status:
Investigational
Source:
NCT01023282: Phase 1 Interventional Completed Parkinson's Disease
(2009)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Ordopidine (also known as ACR-325) is a dopaminergic stabilizer that acts as dopamine D2 receptor antagonists with low affinity. Ordopidine under the development of NeuroSearch participated in phase I trials for the treatment of Parkinson's disease and bipolar disorder. Information about the current study of this drug is not available.
Status:
Investigational
Source:
INN:seridopidine [INN]
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Saniona was developing seridopidine (also known as ACR343), a modulator of dopaminergic activity, as an orally administered therapy for schizophrenia, Tourette's syndrome and parkinson's disease. Seridopidine is a modulator of dopaminergic activity.
Status:
Investigational
Source:
NCT00995345: Phase 2 Interventional Completed Type 2 Diabetes
(2009)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Bisegliptin (also known as KRP-104) was developed as an orally active dipeptidyl peptidase IV (DPPIV) inhibitor. It is known, that DPPIV inhibition reduces blood glucose through suppression of the degradation of the insulin-releasing hormone. Bisegliptin successfully completed the phase II clinical trials for patients with type 2 diabetes. However, further development of the drug has been discontinued for business reason. The company wasn’t able to find a tie-up partner to co-develop.
Class (Stereo):
CHEMICAL (ABSOLUTE)
Sparsomycin is a model protein synthesis inhibitor that blocks peptide bond formation by binding to the large ribosome subunit. It is a unique dipeptidyl alcohol, consisting of a uracil acrylic acid moiety and a monooxo-dithioacetal group. Sparsomycin is a cytotoxic drug exhibiting a broad spectrum of in vitro activity against murine tumors and many tumor cell lines. It also appears to be a potent stimulator of the antitumor activity of cisplatin against L1210 leukemia in vivo. However, because of its toxicity, the antitumor activity of sparsomycin on murine tumors in vivo has been disappointing. Sparsomycin has shown cytostatic activity in a number of in vivo tumor systems, therefore, it was introduced in 1964 in a clinical Phase I study. Two of the five patients of this study developed an ocular toxicity, probably caused by sparsomycin, and so this Phase I study was stopped prematurely.
Status:
Investigational
Source:
NCT02714647: Not Applicable Interventional Completed Basic Motor Learning Problem
(2016)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Status:
Investigational
Source:
NCT04581629: Phase 2 Interventional Completed Autosomal Dominant Hypocalcemia (ADH)
(2020)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Encaleret (JTT-305 or MK-5442) is a potent oral short-acting calcium-sensing receptor (CaSR) antagonist and transiently stimulates endogenous parathyroid hormone (PTH) secretion.
CaSR antagonists stimulate endogenous PTH secretion through CaSR on the surface of parathyroid cells and thereby may be anabolic agents for osteoporosis. Japan Tobacco and Merck were developing encaleret for the treatment of osteoporosis however development has been discontinued.
Status:
Investigational
Source:
NCT03317587: Not Applicable Interventional Completed Obesity
(2017)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
