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Restrict the search for
m nalidixic acid
to a specific field?
Status:
Investigational
Class (Stereo):
CHEMICAL (ACHIRAL)
PBI 4050, a synthetic analog of a medium-chain fatty acid that displays agonist and antagonist ligand affinity toward GPR40 and GPR84, that was developed for managing inflammatory and fibrosis-related diseases. In addition, PBI-4050 may exert antifibrotic activity in the liver through a novel mechanism of action involving modulation of intracellular ATP levels and the LKB1/AMPK/mTOR pathway in stellate cells. This drug participated in clinical trials for the treatment of acute lung injury, cystic fibrosis, diabetic nephropathies; idiopathic pulmonary fibrosis; metabolic syndrome; scleroderma; type 2 diabetes mellitus. Besides, this drug has granted a Rare Pediatric Disease Designation for the treatment of Alström syndrome (AS). PBI-4050 was also previously granted Orphan Drug Designation by the FDA and the EMA for the treatments of AS and idiopathic pulmonary fibrosis (IPF) as well as PIM (Promising Innovative Medicine) designation by the Medicines and Healthcare products Regulatory Agency (MHRA) for the treatment of IPF and AS. The FDA grants Rare Pediatric Disease Designations for serious or life-threatening diseases wherein the serious or life-threatening manifestations primarily affect individuals aged from birth to 18 years, including age groups, often called neonates, infants, children, and adolescents. Now Prometic Life Sciences plans to file investigational new drug application for pivotal phase III trial for Alstrom's syndrome in the second half of 2019.
Status:
Investigational
Class (Stereo):
CHEMICAL (ABSOLUTE)
Conditions:
Sunepitron (CP-93,393) is an anxiolytic drug with highly selective serotonin 5-hydroxytryptamine 1A autoreceptor agonist, alpha2-adrenergic antagonist, and dopamine D2 agonist properties. Sunepitron hydrochloride had been in Phase III clinical trials by Pfizer for the treatment of anxiety disorder and depression. However, this research has been discontinued.
Class (Stereo):
CHEMICAL (ABSOLUTE)
Sparfosate (PALA) is a stable transition state analogue for an aspartate transcarbamylase- cartalyzed reaction with antineoplastic activity. PALA is a potent inhibitor of aspartate transcarbamylase (Ki about 10(-8) M for ACTases of various origins), which in whole cells blocks the de novo synthesis of pyrimidines. Thus PALA inhibits de novo pyrimidine biosynthesis and increases the extent to which fluorouracil metabolites are incorporated into RNA. In vivo, low doses of PALA inhibit whole body pyrimidine synthesis. While this action is cytotoxic in vitro, extensive human testing demonstrates that PALA alone is devoid of selective antitumor activity. Interest in the therapeutic action of PALA derives from the demonstration that its action potentiates the cytotoxicity of several cytotoxic drugs, notably 5-fluorouracil (5-FU). Development of Sparfosate for cancer and Hepatitis B treatment is assumed to have been discontinued.
Status:
Investigational
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Conditions:
Seliciclib (CYC202, R-roscovitine) is a second-generation orally available cyclin-dependent kinases (CDKs) inhibitor that competes for ATP binding sites on these kinases. It is a direct inhibitor of cyclin CDK2/E, CDK2/A and it has inhibitory effects on cyclin H/CDK7, CDK5, and CDK9. CDKs are enzymes that are central to the process of cell division and cell cycle control and play pivotal roles in cancer cell growth and DNA damage repair. Seliciclib exerts an anti-proliferative effect via several key mechanisms: selective downregulation of proliferative and survival proteins and upregulation of p53, leading to growth arrest or apoptosis. The second one is decreasing phosphorylation of Rb and modulating E2F transcriptional activity leading to growth arrest or apoptosis. Seliciclib is currently in phase II clinical trial as a drug candidate for the treatment of Cushing's disease and as a potential therapeutic agent for the treatment of cystic fibrosis (CF). In addition, it is in Phase II trials for non-small cell lung cancer and nasopharyngeal carcinoma.
Class (Stereo):
CHEMICAL (MIXED)
Mexoprofen was studied as an analgesic agent. This compound has never been marketed.
Status:
Investigational
Class (Stereo):
CHEMICAL (ACHIRAL)
Emitefur or BOF-A2 is a fluorinated pyrimidine antimetabolite exerting antineoplastic properties. It is a compound composed of 5-fluorouracil (5-FU) and 3-cyano-2,6-dihydroxypyridine (CNDP), an inhibitor of 5-FU degradation by dihydrouracil dehydrogenase in order to prolong the blood 5-FU level as well as increase selective toxicity to a tumor. Emitefur demonstrated clinical activity in preliminary studies in Japan. Emitefur development for the treatment of solid tumors has been discontinued.
Status:
Investigational
Source:
INN:succinobucol [INN]
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Succinobucol (also known as AGI-1067) is a probucol derivative patented by American pharmaceutical company Atherogenics, Inc as vascular protectant with antioxidant, anti-inflammatory and antiplatelet activities. In vitro, succinobucol inhibits the TNF-α induced expression of VCAM-1 and MCP-1 with little effect on intercellular adhesion molecule (ICAM)-1. In addition, succinobucol inhibits lipopolysaccharide (LPS)-induced expression of tissue factor in human monocytic cells and endothelial cells, an effect thought to be mediated independently from the nuclear factor κB pathway. Preclinical studies have shown reduced total cholesterol and low-density lipoprotein cholesterol concentrations, increased high-density lipoprotein cholesterol concentrations, decreased levels of inflammatory mediators, and reduced atheroma area with Succinobucol treatment in animal models. Unfortunately, in clinical trials, Succinobucol failed to demonstrate a strong cardioprotective effect. Undesired metabolic effects including high-density lipoprotein cholesterol-lowering have been consistently reported, and diarrhea appears to be an expected adverse effect.
Status:
Investigational
Source:
INN:turofexorate isopropyl [INN]
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Conditions:
Turofexorate Isopropyl (XL335) is a potent, selective, and orally bioavailable FXR agonist. Binds to the ligand-binding domain (LBD) of human FXR. Turofexorate Isopropyl resides in a predominately hydrophobic pocket with only a few polar atoms making contact with WAY-362450. Turofexorate Isopropyl promotes transcription of the human BSEP, human SHP, and mouse IBABP genes utilizing reporter constructs with EC50 of 17, 230, and 33 nM, respectively in promoter assays. Turofexorate Isopropyl had been in phase I clinical trials for the treatment of hyperlipidemia. This compound was originally discovered by Exelixis Pharmaceuticals, then licensed to Wyeth (now a wholly-owned subsidiary of Pfizer). However, the studies were discontinued.
Status:
Investigational
Source:
INN:lersivirine [INN]
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
Lersivirine (UK-453,061) is a novel second-generation non-nucleoside reverse transcriptase inhibitor (NNRTI). It binds reverse transcriptase in a distinct way leading to a unique resistance profile. Lersivirine is a second-line NNRTI, which was investigated in a Phase IIb clinical trial. Lersivirine has shown encouraging virologic efficacy in a Phase IIa monotherapy study in NNRTI-naive patients. In a Phase IIb clinical trial in ART naive patients, clinical efficacy of lersivirine was compared with efavirenz, each administered together with tenofovir disoproxil fumarate/emtricitabine. After 48 weeks, lersivirine exhibited a slightly lower virologic response but similar immunologic efficacy. However, the trial was not powered for formal hypothesis testing of noninferiority of lersivirine. The development of lersivirine was recently stopped because the developing company determined that the compound would not provide an improvement over existing NNRTIs.
Class (Stereo):
CHEMICAL (ACHIRAL)
Tiafibrate is a dithiahexadecanediol derivative patented by Juste S. A. Quimico-Farmaceutica as a hypocholesteremic agent. In rats, Tiafibrate at 125 mg/kg day orally for 14 days gave a 38.8% decrease in blood lipids and a 33.7% decrease in blood cholesterol.
