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Restrict the search for
amphotericin b
to a specific field?
Status:
Investigational
Source:
NCT03493607: Phase 2 Interventional Completed Phelan-McDermid Syndrome
(2018)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Diazepinomicin is a structurally novel farnesylated dibenzodiazepinone discovered through DECIPHER technology, Thallion's proprietary drug discovery platform. A small-molecule inhibitor of the RAS/RAF/MAPK signaling pathway with potential antineoplastic activity. Diazepinomicin binds to and inhibits Ras kinase, thereby preventing the phosphorylation and activation of proteins downstream of the Ras signal transduction pathway, including serine/threonine kinase RAF (BRAF) and extracellular signal-regulated kinases 1 and 2 (ERK1 and ERK-2). This agent also selectively binds to the peripheral benzodiazepine receptor (PBR), a receptor highly expressed in certain tumor cell types, inducing cell cycle arrest and apoptosis in PBR-expressing cells. The compound was shown to have a broad cytotoxic activity in the low micromolar range, when tested in the NCI 60 cell line panel. Diazepinomicin can cross the blood-brain barrier. Diazepinomicin is in phase II clinical trials for the treatment of Telomeric 22q13 Monosomy Syndrome and phase I for the treatment of Fragile X syndrome.
Status:
Investigational
Source:
NCT02666001: Phase 1 Interventional Completed Infection, Human Immunodeficiency Virus
(2016)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Norbuprenorphine is a major metabolite of buprenorphine and potent agonist of μ, δ, and κ opioid receptors. Norbuprenorphine is the only known active metabolite of buprenorphine. It has been shown to be a respiratory depressant in rats, but only at concentrations at least 50-fold greater than those observed following application to humans of BuTrans 20 mcg/h. Compared with buprenorphine, norbuprenorphine causes minimal antinociception but greater respiratory depression. In rats, nor-buprenorphine had 1/50th the analgesic potency of buprenor-phine but 10-fold greater respiratory depressant potency. Norbuprenorphine is an in vitro substrate of the efflux transporter P-glycoprotein (Mdr1). Norbuprenorphine is an in vitro and in vivo substrate of P-glycoprotein. P-glycoprotein-mediated efflux influences brain access and antinociceptive, but not the respiratory, effects of norbuprenorphine.
Status:
Investigational
Source:
NCT00062348: Phase 1 Interventional Completed Colorectal Cancer
(2003)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Borocaptate sodium B10 (also known as sodium borocaptate), a boron compound for use in boron neutron capture therapy. After parenteral administration, sodium borocaptate accumulates preferentially in tumor cells. When exposed to neutron irradiation, borocaptate absorbs neutrons and self-destructs releasing short-range alpha radiation and 'recoil' lithium in tumor cells, resulting in alpha radiation-induced tumor cell death. This highly selective, localized radio targeting of tumor cells, known as boron neutron capture therapy, spares adjacent normal tissues. Borocaptate sodium B10 was involved in phase I clinical trial in treating patients with glioblastoma multiforme removed during surgery to study the side effects. In addition, this compound participated in phase I clinical trials in tissues of patients with primary, metastatic, or recurrent thyroid cancer, head and neck cancer, or liver metastases from colorectal cancer to study the side effects. Besides, borocaptate sodium B10 was involved in phase-I clinical trials for Glioma in the European Union, however, this study was discontinued.
Status:
Investigational
Source:
NCT01852604: Phase 2 Interventional Completed Chronic Hepatitis C Virus
(2013)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Samatasvir (also known as IDX 719) was developed by Idenix Pharmaceuticals as a pan-genotypic inhibitor of the hepatitis C (HCV) non-structural protein 5A (NS5A). This drug was studied in phase II clinical trials for the treatment of Hepatitis C, and Chronic Hepatitis C Infection. However, the development of samatasvir was discontinued.
Status:
Investigational
Source:
NCT01359696: Phase 1 Interventional Completed Solid Tumor
(2011)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Status:
Investigational
Source:
NCT01338870: Phase 2 Interventional Completed Diabetes Mellitus, Type 2
(2011)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Conditions:
Pfizer was developing PF-04991532, a potent and selective hepatoselective glucokinase activator. PF-04991532 ameliorates hyperglycemia without causing hepatic steatosis in diabetic rats. F-04991532 reduced plasma glucose concentrations independent of changes in insulin concentrations in a dose-dependent manner both acutely and after 28 days of sub-chronic treatment. PF-04991532 may offer glycemic control without inducing hepatic steatosis supporting the evaluation of tissue specific activators in clinical trials. In 2012, Pfizer discontinued the development of the compound.
Status:
Investigational
Source:
NCT01928537: Phase 3 Interventional Completed Myelodysplastic Syndromes
(2013)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
Rigosertib sodium (ON 01910.Na) is a small molecule inhibitor of critical pathways important in the growth and survival of cancer cells, being developed by Onconova Therapeutics ("Onconova") for the treatment of hematologic malignancies and solid tumors. Rigosertib (ON-01910) is a non-ATP-competitive inhibitor of PLK1 with IC50 of 9 nM in a cell-free assay. It shows 30-fold greater selectivity against Plk2 and no activity to Plk3. Extensive Phase I and Phase II studies with rigosertib have been conducted at leading institutions in the U.S. and abroad in more than 450 patients with solid tumors and hematological cancers, including MDS and AML. MDS and AML are blood disorders widely recognized as difficult to manage, with limited therapeutic options available for patients, especially those with drug-resistant disease. The multi-site Phase III ONTIME trial in MDS patients is under a Special Protocol Assessment (SPA) from the U.S. FDA and is being supported by an award from the Therapeutics Acceleration Program (TAP) of the Leukemia and Lymphoma Society (LLS). FDA has granted Orphan Drug Designation for the use of rigosertib in MDS. The clinical program in solid tumors is also advancing with initiation of the Phase II/III combination ONTRAC trial (ON 01910.Na TRial in Patients with Advanced Pancreatic Cancer) and Phase II single agent trial in ovarian cancer. In Japan, SymBio is developing rigosertib for the treatment of refractory/relapsed HR-MDS (IV form) and first-line LR-MDS (oral form).
Status:
Investigational
Source:
NCT04316546: Phase 2 Interventional Recruiting Proteus Syndrome
(2022)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Miransertib (ARQ 092) is a selective, pan-AKT (protein kinase B) inhibitor that potently inhibits AKT1, 2 and 3 isoforms. Miransertib binds inactive AKT, preventing membrane localization and subsequent AKT activation, and binds active AKT, resulting in direct inhibition. Miransertib participates in Phase 1/2 of clinical trials to treat patients at least 2 years of age with PIK3CA-related Overgrowth Spectrum (PROS) and Proteus syndrome (PS). In addition, the drug is involved in the phase I trial in patients with lymphoma, endometrial cancer, and AKT1 E17K mutations. Recently was shown that miransertib could be an excellent lead compound for the development of new oral drug therapy for visceral and cutaneous leishmaniasis.
Status:
Investigational
Source:
NCT01704495: Phase 2 Interventional Completed Asthma
(2012)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Status:
Investigational
Source:
NCT01351688: Phase 1 Interventional Completed Prostate Cancer
(2011)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Conditions:
AZD-3514 is a down-regulator of androgen receptors. The drug was synthesized by AstraZeneca for the treatment of castrate-resistant prostate cancer and even reached phase I, however, its development was terminated.
