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Restrict the search for
amphotericin b
to a specific field?
Status:
Investigational
Source:
NCT03117920: Phase 2 Interventional Completed Pancreatic Cancer
(2017)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Omtriptolide (previously known as PG490-88 or F60008), an immunosuppressant that has been shown to be the safe and potent antitumor agent and it has been approved entry into Phase I clinical trial for the treatment of prostate cancer in the USA. In addition, the drug is participating in phase I clinical trial for the treatment of myeloid leukemia. Experiments on animals have shown omtriptolide was highly effective in the prevention of murine graft-versus-host disease (GVHD). The immunosuppressive effect of the drug was mediated by inhibition of alloreactive T cell expansion through interleukin-2 production. However, this study was discontinued. Recently published article has shown omtriptolide possesses the potential as a prophylactic agent to prevent ischemia/reperfusion (I/R)-induced lung injury.
Class (Stereo):
CHEMICAL (ABSOLUTE)
Conditions:
Naxagolide (MK-458; L 647,339; (+)-PHNO) is a dopamine D2/D3-receptor agonist, which was studied for the treatment of patients with Parkinson's disease, but further study was discontinued. In addition, was discovered, that Naxagolide C-11 ([(11)C]-(+)-PHNO) was a potential radiotracer for imaging the high-affinity state of dopamine D2 receptors with positron emission tomography (PET) in human subjects. This radiotracer is a suitable for imaging the agonist binding sites (denoted D(2HIGH) and D(3)) of these receptors. PET studies in nonhuman primates documented that, in vivo, [(11)C]-(+)-PHNO displays a relative selectivity for D(3) compared with D(2HIGH) receptor sites and that the [(11)C]-(+)-PHNO signal is enriched in D(3) contribution compared with conventional ligands such as [(11)C] raclopride. Recently was published article reflects the relationship between social attachment and dopamine D2/3 receptor availability in the brains of healthy humans using [11C]-(+)-PHNO.
Class (Stereo):
CHEMICAL (RACEMIC)
Prodolic acid is an indole derivative patented by American Home Products Corp. as antiinflammatory agent. Prodolic acid acts as non-steroidal anti-inflammatory compound and inhibits bradykinin-induced bronchoconstriction but did not affects histamine-induced bronchoconstriction in the guinea pig. In preclinical studies, Prodolic acid exhibits potent anti-inflammatory activity in adjuvant arthritic rats.
Status:
Investigational
Source:
INN:sibopirdine [INN]
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Sibopirdine (EXP921) is a cognition enhancing agent structurally related to linopirdine that was in preclinical development with Bristol-Myers Squibb in the USA as a treatment of Alzheimer's disease. EXP921 was a potential drug candidate for the improvement of cognitive performance in patients with Alzheimer's-type dementia. It has been shown to improve cognitive performance in rodent and primate models of learning and memory. EXP921 was observed to increase the depolarization induced release of acetylcholine, dopamine, and, to a lesser extent, serotonin using slices from the rat cerebral cortex, hippocampus, and caudate nucleus.
Class (Stereo):
CHEMICAL (MIXED)
Tipentosin is prazosin derivative. It is an angiotensin-converting enzyme inhibitor. Tipentosin was developed as an antihypertensive agent.
Status:
Investigational
Class (Stereo):
CHEMICAL (ABSOLUTE)
Sezolamide (previously known as MK-417), a potent carbonic anhydrase inhibitor capable of reducing intraocular pressure after topical application, was under investigation for the treatment of glaucoma. . Sezolamide is the more potent of the two stereo isomers of MK-927 in inhibiting human carbonic anhydrase isoenzyme II, the isoenzyme found in ciliary processes. Sezolamide, the S-enantiomer of MK-927, has demonstrated activity in vitro approximately 80 times that of the R-enantiomer of MK-927 (concentrations of 0.54 nmolll and 44 nM, respectively, inhibiting activity of human carbonic anhydrase isoenzyme II by 50%). Clinically, sezolamide has also demonstrated greater activity than MK-927 both after single-dose and after twice daily administration in
patients.
Status:
Investigational
Source:
USAN:SULFANILATE ZINC [USAN]
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
Sodium sulfanilate is a salt of sulphanilic acid and has been used to monitor the degree of renal dysfunction in dogs.
Status:
Investigational
Source:
NCT00262990: Phase 3 Interventional Completed Ovarian Cancer
(2005)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Patupilone is a compound isolated from the myxobacterium Sorangium cellulosum. Similar to paclitaxel, Patupilone induces microtubule polymerization and stabilizes microtubules against depolymerization conditions. In addition to promoting tubulin polymerization and stabilization of microtubules, this agent is cytotoxic for cells overexpressing P-glycoprotein, a characteristic that distinguishes it from the taxanes. Epothilone B may cause complete cell-cycle arrest. Patupilone failed a phase III trial for ovarian cancer in 2010.
Status:
Investigational
Class (Stereo):
CHEMICAL (ACHIRAL)
Lixazinone selectively inhibits the high-affinity form of cyclic AMP phosphodiesterase (type IV) isolated from human platelets with only weak effects on both the nonspecific and cyclic GMP-sensitive phosphodiesterases. The inhibitor reduces both maximum velocity and substrate affinity of the type IV enzyme. Lixazinone exhibits marked selectively for the platelet high-affinity enzyme. It also has significant inhibitory effects on cardiac membrane-bound phosphodiesterase. Lixazinone may be useful as an agent to increase cardiac output in the treatment of congestive heart failure. It is a potent PDE3 inhibitor. Lixazinone suppresses folic acid-induced proliferation of rat tubular epithelial cells in vivo.
Class (Stereo):
CHEMICAL (ABSOLUTE)
Efepristin (RPR 106972) is an oral streptogramin consisting of two synergistic components RPR 112808 (pristinamycin IB) and RPR 106950 (pristinamycin IIB). It demonstrated activity against Gram-positive microorganisms in vitro and in vivo, including those with multi-drug resistance. The streptogramins inhibit bacterial growth by disrupting the translation of mRNA into protein.
