U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

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Showing 4181 - 4190 of 4705 results

P276-00 (also known as riviciclib) is a novel, potent, small-molecule, flavone-derived inhibitor of cyclin-dependent kinases (Cdk), Cdk 4 D1, Cdk1 B, and Cdk9 T, with potent cytotoxic effects against chemosensitive and chemoresistant cancer cell lines. P276-00 was in phase II clinical trial for the treatment mantle cell lymphoma, but that study was terminated based on interim results and all subjects were off study at that time. Although, there were not the major safety or tolerability concerns. However, this drug successfully passed phase II clinical trial for the treatment Melanoma, squamous cell carcinoma of head and neck, malignant melanoma and in combination with Gemcitabine in the treatment of advanced pancreatic cancer.
Status:
Investigational
Source:
INN:acetorphine
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Acetorphine is a synthetic narcotic analgesic. Acetorphine was reported to have uses in veterinary medicine with pronounced advantages in the immobilization of the giraffe in which toxic effects were reduced as compared to the effects of etorphine. In July 1966, the Director-General of the World Health Organization informed the Secretary-General that WHO had arrived at the conclusion that etorphine and acetorphine should be included in Schedule I of the Convention, since they could give rise to similar abuse, and produce similar ill effects as the substances already listed therein. Acetorphine is a Schedule I controlled substance in the United States.
Status:
Investigational
Source:
NCT02860000: Phase 2 Interventional Active, not recruiting Estrogen Receptor Status
(2017)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Alisertib (MLN8237) is an orally available selective aurora A kinase inhibitor developed by Takeda. Alisertib inhibited AAK over ABK with a selectivity of more than 200-fold in cells and produced a dose-dependent decrease in bipolar and aligned chromosomes in the HCT-116 xenograft model, a phenotype consistent with AAK inhibition. Alisertib inhibited proliferation of human tumor cell lines in vitro and produced tumor growth inhibition in solid tumor xenograft models and regressions in in vivo lymphoma models. It is currently in phase II clinical trials for acute myeloid leukaemia; B cell lymphoma; brain cancer; mesothelioma; prostate cancer; small cell lung cancer.
Status:
Investigational
Source:
INN:cethexonium chloride
Source URL:

Class (Stereo):
CHEMICAL (MIXED)

Cethexonium is a cyclohexanols derivative with antimicrobial activities.
Status:
Investigational
Source:
NCT02260648: Phase 3 Interventional Terminated Hypercholesterolemia
(2015)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Evacetrapib (LY2484595) is a novel benzazepine-based CETP inhibitor that has been developed at Lilly Research Laboratories. Evacetrapib inhibits CETP with IC50 of 5.5 nM, elevates HDL cholesterol without increases in aldosterone or blood pressure. Phase 3. On 01 Sep 2016 Eli Lilly terminates the phase III ACCENTUATE trial in Hyperlipidaemia (Adjunctive treatment) in USA and Puerto Rico (PO) due to insufficient efficacy (NCT02227784).
Status:
Investigational
Source:
NCT04090736: Phase 3 Interventional Active, not recruiting Leukemia, Myeloid, Acute
(2019)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Pevonedistat (MLN4924), discovered by Millennium, is a small molecule inhibitor of the NEDD8-Activating Enzyme (NAE), a key component of the protein homeostasis pathway. MLN4924 is a mechanism-based inhibitor of NAE and creates a covalent NEDD8-MLN4924 adduct catalyzed by the enzyme. The NEDD8-MLN4924 adduct resembles NEDD8 adenylate, the first intermediate in the NAE reaction cycle, but cannot be further utilized in subsequent intraenzyme reactions. The stability of the NEDD8-MLN4924 adduct within the NAE active site blocks enzyme activity, thereby accounting for the potent inhibition of the NEDD8 pathway by MLN4924. This drug is in phase II clinical trial for the treatment acute myeloid leukemia, chronic myelomonocytic leukemia and myelodysplastic syndromes. In addition in phase I for treatment acute lymphoblastic leukemia. The ability of MLN4924 to cross the blood-brain barrier, its low toxicity, and clinical efficacy in other cancers suggests that this drug is an attractive treatment against glioblastomas.
Status:
Investigational
Source:
NCT00805805: Phase 3 Interventional Completed Primary Biliary Cirrhosis
(2006)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Status:
Investigational
Source:
NCT01110499: Phase 2 Interventional Completed Ocular Hypertension
(2010)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Aganepag isopropyl, an IOP-lowering agent, is an antiglaucoma agent. It is a selective EP2 receptor agonist.
Status:
Investigational
Source:
NCT01110499: Phase 2 Interventional Completed Ocular Hypertension
(2010)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Aganepag isopropyl, an IOP-lowering agent, is an antiglaucoma agent. It is a selective EP2 receptor agonist.
Status:
Investigational
Source:
INN:profadol
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Profadol is a pyrrolidine derivative patented in the 1960s by pharmaceutical company Parke-Davis as opioid analgesic. Profadol acts as a mixed agonist-antagonist of the μ-opioid receptor and in preclinical studies, Profadol precipitates abstinence in morphine-dependent monkeys and can reverse pethidine- induced narcosis in nondependent monkeys. In morphine-dependent human subjects, Profadol was also found to pre¬cipitate acute abstinence syndromes, with a potency 40 to 50 times less than that of nalorphine. Profadol, unlike other morphine-antagonists, does not produce nalorphine-like subjective effects. Over a fourfold range of doses, this drug was found to produce subjective effects indistinguishable from those of morphine. Also unlike other morphine-antagonists, profadol is quite active on the "classical" rodent tests for analgesia. It is about 1.3 times as potent as pethidine on the mouse hot-plate test, and about four times as potent on the rat tail-pressure test.

Showing 4181 - 4190 of 4705 results