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Restrict the search for
angiotensin ii
to a specific field?
Status:
Investigational
Source:
NCT03592472: Phase 3 Interventional Recruiting Renal Cell Carcinoma
(2018)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Conditions:
Abexinostat (PCI-24781) is a novel, second-generation phenyl hydroxamic acid–based, orally bioavailable HDAC inhibitor that has previously been shown to have activity in vitro and in vivo against a broad array of cancers, including hematopoietic malignancies and bone and soft-tissue sarcomas. Abexinostat is a pan-HDAC inhibitor mostly targeting HDAC1 with Ki of 7 nM, modest potent to HDACs 2, 3, 6, and 10 and greater than 40-fold selectivity against HDAC8. Abexinostat exhibits potent antitumor activity against a variety of tumor cell lines with GI50 ranging from 0.15 uM to 3.09 uM. PCI-24781 also has an antiproliferative effect on HUVEC endothelial cells with GI50 of 0.43 uM. Abexinostat treatment causes dose-dependent accumulation of both acetylated histones and acetylated tubulin in HCT116 or DLD-1 cells, induces expression of p21, and leads to PARP cleavage and accumulation of the γH2AX. It has also shown good tolerability and activity in Phase I and II clinical trials against lymphoma, as well as against solid tumors in Phase-I trials. Additionally, it acts as a potent radiosensitizing agent and is synergistic with cytotoxic chemotherapy, such as doxorubicin in preclinical models.
Status:
Investigational
Source:
NCT01628094: Phase 2 Interventional Completed Hepatitis C, Chronic
(2012)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Conditions:
Mericitabine is a specific inhibitor of hepatitis C virus (HCV) replication that target NS5B polymerase. Mericitabine, a prodrug, is hydrolyzed in vivo to produce PSI-6130. It had been studied in phase II clinical trials for the treatment of chronic hepatitis C. However, while it showed a good safety profile in clinical trials, it was not sufficiently effective to be used as a standalone agent.
Status:
Investigational
Source:
NCT01218204: Phase 2 Interventional Completed Dyslipidaemias
(2010)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Conditions:
GSK1292263 (GSK263) (5-[({1-[3-(1-methylethyl)-1,2,4-oxadiazol-5-yl]-4-piperidinyl}methyl)oxy]-2-[4-(methylsulfonyl)phenyl]pyridine) is a potent and selective agonist at the rodent and human GPR119 receptors that was discovered at GlaxoSmithKline. It has a pEC50 = 6.8 for human, rat and mouse GPR119 receptors expressed in an in vitro reporter assay, and a pEC50 = 8.5 for the stimulation of GLP-1 secretion from GLUTag cells. Like other GPR119 agonists, GSK1292263 increases glucose-sensitive insulin secretion, improves glucose tolerance and enhances the secretion of gut hormones in normal rats. GSK1292263 has finished Phase II clinical trial for Diabetes Mellitus, Type 2.
Status:
Investigational
Source:
NCT00843518: Phase 2 Interventional Completed Alzheimer's Disease
(2009)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Conditions:
Mibampator, also known as LY451395, is a potent and highly selective an AMPA receptor potentiator, which plays a role in the regulation of the glutamatergic system. The AMPA system also has important functions in the regulation of synapses, synaptic regeneration, and neuroprotection and is therefore a good therapeutic target for treatments aiming to improve cognition and function or alter disease progression. Mibampator was in the phase II clinical trial for the treatment of agitation and aggression in Alzheimer's disease (AD).
Status:
Investigational
Source:
NCT02509546: Phase 1/Phase 2 Interventional Completed Acute Myeloid Leukemia Arising From Previous Myelodysplastic Syndrome
(2015)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
8-chloroadenosine (8-Cl-Ado) is a ribonucleoside analog. The mechanism of its action remains poorly understood, however, it is known that the drug inhibits RNA synthesis. It has significant cytotoxic activity against lymphoid and myeloid malignant cells. The nucleoside analog 8-Cl-Ado is phosphorylated into its cytotoxic triphosphate 8-Cl-ATP. The accumulation of the cytotoxic metabolite results in a parallel decrease of the ATP cellular pools. 8-Cl-Ado gets incorporated into RNA during transcription, hindering this process. In addition, this triphosphate inhibits ATP-dependent poly(A) tail synthesis, and, as a consequence, mRNA processing is inhibited, resulting in vitro cytotoxicity in several solid and hematological malignancies. This agent is currently in clinical trials for the treatment of chronic lymphocytic leukemia and acute myeloid leukemia.
Status:
Investigational
Source:
NCT00558662: Not Applicable Interventional Completed Venous Ulcer
(2007)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Status:
Investigational
Source:
NCT04697810: Phase 2 Interventional Recruiting NASH - Nonalcoholic Steatohepatitis
(2021)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
CF102 known as Cl-IB-MECA (2-chloro-N6-(3-iodobenzyl)-adenosine-5’- N-methyl-uronamide), is a highly specific and selective agonist at the A3 adenosine receptor. Phase I/II study in hepatocellular carcinoma (HCC) successfully met its primary and secondary endpoints demonstrating initial indications for efficacy of CF102. A global Phase II study treating patients with CF102 as a second line therapy will start enroling patients shortly.
Status:
Investigational
Source:
NCT01294202: Phase 2 Interventional Completed Gastrointestinal Stromal Tumor (GIST)
(2011)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Onalespib (AT13387; (2,4-dihydroxy-5-isopropyl-phenyl)-[5-(4-methyl-piperazin-1-ylmethyl)-1,3-dihydro-isoindol-2-yl] methanone, l-lactic acid salt), is wholly owned by Astex, a novel, high-affinity HSP90 inhibitor, which is currently being clinically tested, has shown activity against a wide array of tumor cell lines, including lung cancer cell lines. As a targeted inhibitor of Hsp90, onalespib has the potential to control the proliferation of multiple solid tumors and hematological malignancies where uncontrolled cell growth is dependent on the interaction between Hsp90 and its client proteins. Astex is pursuing an approach based on the observation that addition of onalespib to a molecularly targeted agent may delay the emergence of resistance to the agent, and hence prolong the window of therapeutic benefit. Onalespib is currently being evaluated via a CRADA with the National Cancer Institute (NCI) in various tumor types, and in a Phase 1/2 clinical study in combination with AT7519, Astex CDK inhibitor.
Status:
Investigational
Source:
NCT03070132: Phase 3 Interventional Withdrawn Trigeminal Neuralgia
(2023)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Raxatrigine also known as GSK1014802 and CNV-1014802, is a novel analgesic under development by Convergence Pharmaceuticals for the treatment of lumbosacral radiculopathy (sciatica) and trigeminal neuralgia (TGN). It is a novel state dependent small molecule sodium channel blocker that preferentially inhibits the Nav 1.7 ion channel, a therapeutic target implicated by genetics in human pain conditions. Raxatrigine is thought to penetrate the central nervous system and block Nav channels in a novel manner. CNV1014802 was granted orphan drug designation in 2013 by the US Food and Drug Administration (FDA) for the treatment of trigeminal neuralgia.
Status:
Investigational
Source:
NCT02756130: Phase 1/Phase 2 Interventional Withdrawn High Grade Fallopian Tube Serous Adenocarcinoma
(2018)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Conditions:
Birinapant is a parenterally administered bivalent peptidomimetic of the SMAC protein (Second Mitochondria-derived Activator of Caspases) and is therefore known as a SMAC mimetic compound. Birinapant is a particularly potent antagonist of two members of the Inhibitor of Apoptosis Proteins (IAP) family, cIAP-1, and cIAP-2. cIAP-1 and -2 are ubiquitin ligases whose expression can protect cells from apoptosis and cause pro-survival effects of TNF-α and related ligands. When Birinapant binds to cIAP-1 or -2 it causes the protein to ubiquitinate itself, which in turn drives the degradation of the protein. In this way, birinapant suppresses the levels of cIAP-1 and cIAP-2 and therefore switches cell signaling to drive tumor cell apoptosis in the presence of TNF-α. Birinapant has been shown to give rise to sustained and substantial reductions of cIAP1 levels in Peripheral Blood Mononuclear Cells (PBMCs) and tumor tissue. To date, Birinapant has been dosed in approximately 450 patients across 9 studies. The majority of studies was in oncology (one in HBV) and primarily recruited patients with refractory solid tumors & hematological malignancies (dominated by ovarian, colorectal, acute myeloid leukemia and Myelodysplastic syndromes). Overall Birinapant has shown acceptable safety and tolerability for further development in oncology indications. The current plans are to study Birinapant clinically in combination with Keytruda® for the treatment solid tumors and in an Investigator-Initiated study at UCLA for high-grade serous carcinoma (HGSC) in combination with platinum-based chemotherapy.
