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Restrict the search for
m nalidixic acid
to a specific field?
Status:
Investigational
Source:
NCT01528111: Phase 1/Phase 2 Interventional Completed Primary Open-angle Glaucoma
(2012)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
LX-7101 (Lexicon Pharmaceuticals) was advanced to Phase-I clinical trials for treatment open-angle glaucoma or ocular hypertension. This drug is a potent inhibitor of LIM-kinase 2 (LIMK2) kinase and inhibits to less extent LIMK1 and Rho-associated protein kinase 2 (ROCK2).
Status:
Investigational
Source:
NCT03926624: Phase 3 Interventional Recruiting Leukemia, Myeloid, Acute
(2019)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
CNDAC (TAK-109) is an analog of the nucleoside deoxycytidine with potential antineoplastic activity. CNDAC is incorporated into DNA and induces single-strand breaks, which are converted into double-strand breaks (DSBs) when cells go through a second S phase. This results in the cell cycle arrest in the S and G2/M phases, DNA fragmentation, and tumor cell apoptosis. Sapacitabine, a prodrug of CNDAC, is being developed by the US biotechnology company Cyclacel for the treatment of hemalogical cancers and solid tumors.
Status:
Investigational
Source:
NCT01306903: Not Applicable Interventional Completed Postoperative Bloodloss
(2011)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Status:
Investigational
Source:
NCT01971385: Phase 1 Interventional Completed Herpes Labialis
(2013)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Squaric acid is a dibasic organic acid and useful intermediate in a variety of synthetic reactions involving the synthesis of photosensitive squarylium dyes and inhibitors of protein tyrosine phosphatases. Medically, squaric acid dibutyl ester or dibutyl squarate derives from a squaric acid is used for the treatment of warts.
Status:
Investigational
Source:
NCT01320787: Phase 1 Interventional Withdrawn Brain Cancer
(2014)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Fluoroacetic acid F-18 (18F-Fluoroacetate,18F-FAC) is an analog of acetate with a longer radioactive half-life (18F=110 min). Fluoroacetic acid F-18 was under investigation as a PET imaging agent. 18F-FAC was considered a promising alternative to 11C-ACE for positron tomographic imaging of prostate cancer, and possibly of other neoplasms with relatively low glucose use.
Status:
Investigational
Source:
NCT02226549: Phase 2 Interventional Completed Hepatitis C Virus Infection
(2014)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Vedroprevir, or GS-9451, is a potent inhibitor of the HCV NS3 protease (Box 1). NS3 is a serine protease that cleaves the HCV polyprotein and helps generate the viral replication complex. Through binding NS3, vedroprevir halts the assembly of the viral replication complex, thus interfering with the assembly and release of viral particles. Vedroprevir is a potent inhibitor of NS3 protease with high selectivity against off-target proteases. It has rapid association kinetics and slow dissociation kinetics. Preclinical studies of vedroprevir showed high oral bioavailability in rats, dogs, and monkeys. Preclinical studies of vedroprevir demonstrated potent NS3 inhibition using laboratory strains as well as patient-derived NS3 protease gene isolates. In a phase I, randomized trial of vedroprevir monotherapy, doses of 200 and 400 mg/day yielded median maximal HCV RNA reductions of −3.2 log10 in genotype 1a patients and −3.5 log10 in genotype 1b patients. Significantly less activity was seen against genotype 2a HCV when compared to genotype 1. Vedroprevir was not listed on the Gilead Sciences pipeline in its 2014 annual report and appears to have been discontinued for the once-daily treatment of Hepatitis C.
Status:
Investigational
Source:
INN:sodium iotalamate (¹³¹I) [INN]
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Status:
Investigational
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
4,4’-Diamino-2,2’-stilbenedisulfonic acid (also known as amsonic acid) is used in the synthesis of dyes and optical brighteners or fluorescent whitening agents. Amsonic acid possesses estrogenic activity, and thus provided a possible mechanistic explanation for the complaints of impotency in factory workers exposed to this compound. In the 2-year feed studies on rodents, there was no evidence of carcinogenic activity of amsonic acid, in male or female F344/N rats receiving 12,500 or 25,000 ppm. In addition, there was no evidence of carcinogenic activity of this compound in male or female B6C3F1 mice receiving 6,250 or 12,500 ppm.
Status:
Investigational
Source:
NCT01020006: Phase 2 Interventional Completed Pancreatic Cancer
(2009)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Conditions:
PCI-27483 is a reversible small-molecule inhibitor of activated factor VII (factor VIIa) with potential antineoplastic and antithrombotic activities. FVII, a serine protease, becomes activated (FVIIa) upon binding with TF forming the FVIIa/TF complex, which induces intracellular signaling pathways by activating protease activated receptor 2 (PAR-2). Upon subcutaneous administration, factor VIIa inhibitor PCI-27483 selectively inhibits factor FVIIa in the VIIa/TF complex, which may prevent PAR-2 activation and PAR2-mediated signal transduction pathways, thereby inhibiting tumor cell proliferation, angiogenesis, and metastasis of TF-overexpressing tumor cells. A phase I study in healthy volunteers was conducted
to assess the PD and PK profiles of PCI-
27483 following a single, SC injection. The halflife
of PCI-27483 was 10-12 h. The International
Normalized Ratio (INR) was strongly correlated
with drug plasma concentration. PCI-27483 was
well tolerated. This compound has being evaluated in a phase Ib/II trial in patients with pancreatic cancer receiving treatment with gemcitabine. However, no recent development has been reported. The compound was originally developed by Celera, then licensed to Pharmacyclics (acquired by Abbvie in 2015) later.
In 2012, the product was licensed to Novo Nordisk by Pharmacyclics for disease outside of oncology.
Status:
Investigational
Source:
NCT01551147: Phase 2 Interventional Completed Asthma
(2012)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Gemilukast (ONO-6950) is an orally active compound that has been evaluated for the treatment of asthma. It is an CysLT1 and CysLT2 antagonist. Activation of CysLT2 receptors has been suggested to contribute to antigen-induced bronchoconstriction (constriction of the airways in the lungs) in certain asthma patients. In addition to its CysLT1 and CysLT2 antagonist activity, Gemilukast was shown to dose-dependently reduce LTC4-induced bronchoconstriction in asthmatic models, and reduce antigen-induced constriction of isolated human bronchi. A phase II trial with Gemilukast was discontinued in 2018.
