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

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Showing 201 - 210 of 2738 results

Status:
Investigational
Source:
Eur J Cancer Clin Oncol. May 1986;22(5):601-5.: Phase 2 Human clinical trial Completed Breast Neoplasms
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Carubicin (also known as Carminomycin) is an anthracycline antineoplastic antibiotic isolated from the bacterium Actinomadura carminata. Carubicin intercalates into DNA and interacts with topoisomerase II, thereby inhibiting DNA replication and repair and RNA and protein synthesis. The drug is active against a variety of experimental tumors. Pharmacology studies in animals revealed that the drug bound largely to serum proteins and that it was widely distributed. In clinical trials The main toxic effect was myelosuppression but gastrointestinal intolerance and alopecia were also reported. Objective partial responses were seen in two of seven previously untreated patients with non-small cell lung cancer and one of three patients with squamous cell carcinoma of the head and neck previously untreated with chemotherapy.
Status:
Investigational
Source:
INN:diacetolol
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Diacetolol is the major metabolite of the β-adrenoceptor blocking agent, acebutolol. In vitro, the β-adrenoceptor blocking potency of diacetolol was less than that of acebutolol but its cardioselectivity (atrial relative to tracheal tissue) was greater. Diacetolol had weak intrinsic sympathomimetic activity, and no significant membrane-stabilizing activity. It did not restore sinus rhythm to anaesthetized dogs with ouabain-induced arrhythmias but was similar to acebutolol in preventing arrhythmia induced by adrenaline/methylchloroform in anaesthetized cats. Study of diacetolol pharmacokinetics and bioavailability suggests either a first-pass effect or incomplete absorption of diacetolol after oral administration. Diacetolol plasma half-life after oral administration is about 12 h and is not dose-dependent. Diacetolol possesses significant antihypertensive action against moderate essential hypertension in man. Its antihypertensive effect is associated with a reduction in the heart rate and a decrease in plasma renin activity.
Status:
Investigational
Source:
INN:bencisteine
Source URL:

Class (Stereo):
CHEMICAL (EPIMERIC)

Bencisteine was developed as an antitussive, mucolytic agent.
Status:
Investigational
Source:
NCT01092689: Phase 1 Interventional Withdrawn Pancreas Cancer
(2012)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

2-Amino-1-methyl-6-phenylimidazo[4,5-b]pyridine (PhIP) is a mutagenic and carcinogenic heterocyclic amine formed during ordinary cooking, and is subsequently metabolically activated by cytochrome P4501A2 (CYP1A2) and N-acetyltransferase 2 (NAT2). PhIP has been used in trials studying the basic science of Pancreas Cancer.
Status:
Investigational
Source:
NCT01766622: Phase 2 Interventional Withdrawn Ovarian Neoplasms
(2012)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Status:
Investigational
Source:
Oncology. 2005;69(1):19-26.: Phase 3 Human clinical trial Completed Lymphoma, Non-Hodgkin/pathology
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Status:
Investigational
Source:
INN:cefmepidium chloride
Source URL:

Class (Stereo):
CHEMICAL (EPIMERIC)

Cefmepidium is a semisynthetic cephalosporin with broad antibacterial activity against penicillin-resistant strains.
Status:
Investigational
Source:
NCT03833362: Phase 3 Interventional Completed Hepatitis C
(2014)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


Narlaprevir (formerly SCH 900518), a NS3 protease inhibitor is being developed by R-Pharm for the treatment of a chronic hepatitis C (genotype 1). Narlaprevir is a potent inhibitor of hepatitis C virus (HCV) NS3 protease with a Ki of 7 ± 1 nM and a 90% inhibitory concentration (IC90) of ∼28 ng/ml for HCV genotype 1 replicon in vitro. Narlaprevir successfully passed extensive pre-clinical and clinical trials in Schering-Plough Research Institute (USA) and in a variety of clinical centers of Europe, USA and Russia. Based on clinical findings R-Pharm obtained a registration certificate for Arlansa (Narlaprevir) ЛП-003622 dd 12.05.2016 issued by Ministry of Healthcare of the Russian Federation.
Status:
Investigational
Source:
NCT02124447: Not Applicable Interventional Withdrawn Patients Undergoing Screening or Surveillance Colonoscopy
(2014)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

N-Acetylsulfanilyl chloride is a benzenesulfonyl chloride derivative used as intermediate in the synthesis of various pharmaceuticals and organic compounds. N-Acetylsulfanilyl chloride is also used in the synthesis of N,N-dimethylsulfanilamide as the internal standard in the reaction. The reaction is used to determine tramadol and its O-demethylated metabolite in blood plasma.
Status:
Investigational
Source:
NCT00504790: Phase 1 Interventional Completed Cancer
(2007)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


Conditions:

GSK-923295 is a small-molecule inhibitor of the mitotic kinesin centromere-associated protein E (CENP-E), and the third novel drug candidate to arise from Cytokinetics' broad strategic alliance with GlaxoSmithKline (GSK). GSK-923295 demonstrated a broad spectrum of activity against a range of human tumor xenografts grown in nude mice, including models of colon, breast, ovarian, lung and other tumors. GSK-923295 is the first drug candidate to enter human clinical trials that specifically targets CENP-E and is currently in Phase I human clinical trials being conducted by GSK. GSK-923295 inhibited release of inorganic phosphate and stabilized CENP-E motor domain interaction with microtubules. Inhibition of CENP-E motor activity in cultured cells and tumor xenografts caused failure of metaphase chromosome alignment and induced mitotic arrest, indicating that tight binding of CENP-E to microtubules is insufficient to satisfy the mitotic checkpoint. Consistent with genetic studies in mice suggesting that decreased CENP-E function can have a tumor-suppressive effect, inhibition of CENP-E induced tumor cell apoptosis and tumor regression.