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Restrict the search for
sulfisoxazole acetyl
to a specific field?
Status:
Investigational
Source:
INN:ansornitinib [INN]
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Status:
Investigational
Source:
NCT02489461: Phase 2/Phase 3 Interventional Completed HIV-1-infection
(2014)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
R-1206 (also known as Elsulfavirine) is a phenylacetamide derivative patented by Roche Palo Alto LLC as non-nucleoside reverse transcriptase inhibitor (NNRTI) for treating retroviral infections. R-1206 is the prodrug of the active compound VM-1500A, a small molecule selective NNRTI, which prevents HIV replication. The antiviral activity of R-1206 is broad, with activity demonstrated towards various viral strains and clinical isolates of HIV, including those resistant to other NNRTIs. Furthermore, R-1206 was associated with a low probability of cross-resistance or resistance development, and a high genetic barrier to the development of resistant drug mutations. In clinical trials, R-1206 20 and 40 mg demonstrated superiority to efavirenz in terms of the effectiveness to reduce the level of viral load to 400 copies/mL after 12 weeks of therapy. R-1206 20 mg once daily is generally well tolerated in ART-naive HIV-1 infected patients.
Status:
Investigational
Source:
NCT04486911: Phase 2 Interventional Active, not recruiting Breast Cancer
(2020)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
Donitriptan hydrochloride (F 11356) was developed by Pierre Fabre as a brain penetrant 5-HT1B/1D agonist. Which inhibits capsaicin-induced external carotid vasodilation and produces selective carotid vasoconstriction in various animal species. In January 2001, donitriptan had completed phase I trials for migraine and was scheduled to enter phase II development, but before development in phase II, this drug was discontinued.
Status:
Investigational
Class (Stereo):
CHEMICAL (RACEMIC)
Targets:
Otenzepad is the first competitive muscarinic M2 antagonist that is cardioselective and had been in phase III clinical trials for the treatment of arrhythmias and bradycardia. Otenzepad was originally developed by Boehringer Ingelheim Pharma KG (Boehringer Ingelheim) in Germany. The parent company is developing oral and IV formulations of the drug for use in symptomatic bradycardia, sinus bradycardia, sick sinus syndrome and symptomatic arrhythmias after intoxication. However, all these research has been discontinued. Otenzepad binds to muscarinic cholinergic receptors in a simple competitive manner. Its affinity for cardiac (M2) muscarinic receptors is about 7 times greater than for ganglionic (M1) receptors and about 36 times greater than for glandular (M3) receptors. The (+)-enantiomer of otenzepad is about 8 times more potent at M2-receptors than the (−)-enantiomer. In a double-blind study, 48 healthy male volunteers were randomised to single oral doses of placebo or otenzepad (120, 240 or 480mg). Heart-rate (HR) was significantly increased by the 250 and 480mg doses (by 15 and 21 beats/minute, respectively). The 480mg dose also increased Diastolic Blood Pressure (DBP) significantly compared with placebo. The oral pharmacokinetics of otenzepad were investigated in a double-blind study in which 48 healthy male volunteers were randomised to single oral doses of placebo or otenzepad (120, 240 or 480mg). Otenzepad bioavailability was 45%, mean residence time (MRT) was 12.5 hours and tmax occurred 2.5 hours postdose.
Status:
Investigational
Source:
NCT03781947: Phase 1 Interventional Completed Healthy
(2018)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Teverelix is a polypeptide gonadotropin-releasing hormone (GnRH) antagonist which was being developed by Ardana Bioscience for the treatment of prostate cancer and benign prostatic hyperplasia. Compared with other GnRH antagonists, Teverelix is characterized by relatively good water solubility, little in vitro aggregation, and low histamine-releasing potency, with a dose that produces the halfmaximal response. In preclinical studies, Teverelix has been shown to exert antiovulatory activity. In phase I clinical trials Teverelix shows pronounced luteinizing hormone and testosterone suppressive effects after single subcutaneous doses in healthy men.
Status:
Investigational
Source:
NCT03457948: Phase 2 Interventional Active, not recruiting Metastatic Malignant Neoplasm in the Liver
(2018)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Status:
Investigational
Source:
NCT01125644: Phase 3 Interventional Unknown status Cryptococcosis or Aspergillosis Infections
(2010)
Source URL:
Class (Stereo):
CHEMICAL (EPIMERIC)
SPK-843 is a water-soluble partricin derivative patented by SPA Societa Prodotti Antibiotici S.p.A. and developed by Aparts and Kaken for the potential treatment of systemic fungal infections. In preclinical models, SPK-843 shows in vitro inhibitory activity comparable to or better than that of Amphotericin B against Candida spp., Cryptococcus neoformans, and Aspergillus spp. SPK-843 exhibits dose-dependent efficacy on murine pulmonary aspergillosis models. SPK-843 doses of higher than 1.0 mg/kg of body weight exhibit no renal toxicities and a tendency toward better survival prolongation than the estimated maximum tolerated doses of amphotericin B (Fungizone) and liposomal amphotericin B.
Class (Stereo):
CHEMICAL (ABSOLUTE)
Detirelix is a synthetic decapeptide containing five D-amino acids. It is a very potent Gonadotropin-releasing hormone (GnHR) antagonist. The acute effects of detirelix were consistent with peripheral vasodilation. Subchronic effects were associated with inhibition of pituitary gonadotropic and gonadal hormone secretion. As long-acting GnRH antagonist detirelix can rapidly suppress gonadotropin secretion, inhibit follicular development, and prevent ovulation. It can be used as luteolytic agent. A projected use is for the treatment of sex hormone-releasing diseases, as part of anticancer hormone therapy of sex-hormone-dependent tumors.
Status:
Investigational
Source:
INN:atuzaginstat [INN]
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
