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

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Showing 201 - 210 of 9567 results

Status:
Investigational
Source:
INN:trospectomycin
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Trospectomycin is an aminocyclitol antibiotic similar in structure to spectinomycin. The drug was originally developed by Pharmacia & Upjohn. It is a 6'-propyl analogue of spectinomycin, and lacks the aminosugars in glycosidic linkage which are thought to be responsible for the ototoxicity and nephrotoxicity associated with the aminoglycosides. The mechanism of action of trospectomycin is similar to that of its parent compound, spectinomycin: it binds to the bacterial 30S ribosome and inhibits protein synthesis. The transport mechanism for its delivery to its target site does not appear to be oxygen dependent, and this explains the in-vitro activity of trospectomycin against anaerobic organisms. Trospectomycin has activity against a broad spectrum of pathogenic organisms including Streptococcus, Haemophilus, Gardnerella, Neisseria, Peptococcus, Peptostreptococcus, Bacteroides, Mobiluncus, Chlamydia, Mycoplasma and Ureaplasma spp. Results of in-vivo testing suggest potential utility in a variety of clinical conditions including non-gonococcal urethritis, chlamydial cervicitis, gonorrhoea, pelvic inflammatory disease, pneumonia, anaerobic infections and meningitis. Trospectomycin progressed to late stage clinical trials for treatment of pelvic inflammatory disease (chlamydia) before being abandoned for commercial reasons as the third generation cephalosporins and second generation macrolides in development and use were judged superior at the time.
Status:
Investigational
Source:
INN:idoxifene
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Idoxifene (also known as CB 7432), a novel selective estrogen receptor modulator, is originally discovered at the CRC Centre for Cancer Therapeutics, Institute. This drug participated in clinical trials phase II in patients with locally advanced/metastatic breast cancer resistant to tamoxifen. In addition, in phase III in postmenopausal women after one year of idoxifene treatment. However, both studies were discontinued because of insufficient effectiveness.
Status:
Investigational
Source:
INN:mibolerone
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


Conditions:

Mibolerone is a synthetic anabolic steroid. It binds both androgen and progesterone receptors and exerts both androgenic and progestagenic actions. Mibolerone (CHEQUE® Drops) was used in veterinary for estrous (heat) prevention in adult female dogs not intended primarily for breeding purposes. No prescription preparation, human or veterinary, is currently known to contain mibolerone worldwide.
Status:
Investigational
Source:
INN:cinoxolone
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Cinoxolone is a derivative of glycyrrhetinic acid. Is is claimed to possess antiulcer properties.
Status:
Investigational
Source:
INN:mofegiline
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Mofegiline (MDL 72,974A or (E)-2-(4-fluorophenethyl)-3-fluoroallylamine, hydrochloride), is a selective and irreversible inhibitor of monoamine oxidase type B (MAO-B) both in vitro and in vivo. In addition, mofegiline inhibits semicarbazide-sensitive amine oxidase activity from human serum and saphenous vein. In phase II studies, MDL 72,974A is proving to be a useful adjunct to conventional therapy of Parkinson's disease. It seems mofegiline development was discontinued.
Status:
Investigational
Source:
USAN:Actodigin
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Actodigin is a semisynthetic cardiac glycoside compounded from digitoxigenin and one molecule of glucose. In addition, unlike the naturally occurring glycosides, the C-2 instead of the C-3 atom of the lactone ring is attached to the steroid nucleus. Actodigin is a cardiovascular agent. When injected at 30 min invervals into dogs with barbiturate-induced heart failure, actodigin caused a marked positive inotropic action of short duration. It converted arrhythmia to normal sinus rhythm. Actodigin effectively and quickly reduced the ventricular rate in patients with atrial fibrillation. Actodigin, because of its rapid onset and brief duration of action, may be useful in controlling the ventricular rate in patients with atrial fibrillation.
Status:
Investigational
Source:
INN:edotecarin [INN]
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Edotecarin (J-107088 or [6-N-(1-hydroxymethyl-2-hydroxy)ethylamino-12,13-dihydro-2,10-dihydroxy- 13-(beta-D-glucopyranosyl)-5H-indolo[2,3-a]-pyrrolo[3,4-c]-carb azo le-5,7(6H)-dione]) is a DNA topoisomerase I inhibitor. The antitumor activity of edotecarin has been tested in vitro and in vivo, and inhibition of tumor growth has been observed in breast, cervix, pharynx, lung, prostate, colon, gastric, and hepatic cancer models. Banyu Pharmaceutical Co Ltd and Pfizer Inc were developing edotecarin for the potential treatment of solid tumors. Edotecarin development has been discontinued.
Status:
Investigational
Source:
INN:lanabecestat [INN]
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


AZD-3293 camsylate wider known as Lanabecestat camsylate, a salt of Lanabecestat, a drug that was invented for the treatment of Alzheimer's disease. Lanabecestat inhibits beta-secretase 1 cleaving enzyme (BACE1) thus preventing the buildup of beta-amyloid and help stop the progression of Alzheimer's disease. The drug was in phase III clinical trials, but studies were discontinued because of recommendations by an independent data monitoring committee (IDMC). IDMC concluded that all trials, in early Alzheimer’s disease, and in mild Alzheimer’s disease dementia, were not likely to meet their primary endpoints upon completion and therefore should be stopped for futility.
Status:
Investigational
Source:
INN:lidimycin
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Lydimycin is a biosynthetic product obtained by culturing a lydimycin-producing actinomycete in a suitable aqueous nutrient medium under aerobic conditions. Lydimycin inhibits the growth of Nocardia asteroides, Blastomyces dermatitidis, Geotrichum sp., Phlalophora varrucosa, Cryptococcus neoformans, H Histoplasma capsulatum, and Trichophyton mentagrophytes. Thus, lydimycin is useful alone or in combination with other antifungal or antibiotic agents to prevent the growth of, or reduce the number of, susceptible organisms present in various environments.
Status:
Investigational
Source:
NCT03593226: Phase 1/Phase 2 Interventional Completed Superficial, Palpable, Unresectable/Metastatic Solid Tumour
(2018)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)