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

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Showing 201 - 210 of 693 results

Status:
Investigational
Source:
INN:mofarotene
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Mofarotene is an analog of retinoic acid patented by a Swiss multinational healthcare company Hoffmann-La Roche as neoplasm inhibitors and agent for treating dermatoses. Like other retinoic acid agents, mofarotene binds to and activates retinoic acid receptors (RARs), thereby altering the expression of certain genes leading to cell differentiation and decreased cell proliferation in susceptible cells. Mofarotene has demonstrated considerable antitumor activity in a number of cancer cell lines. Mofarotene in combination with cisplatin and etoposide was studied in phase I clinical trials but further development was discontinued.
Fenretinide (4-HPR) is an orally-active synthetic phenylretinamide analogue of retinol (vitamin A) with potential antineoplastic and chemopreventive activities. Fenretinide binds to and activates retinoic acid receptors (RARs), thereby inducing cell differentiation and apoptosis in some tumor cell types. This agent also inhibits tumor growth by modulating angiogenesis-associated growth factors and their receptors and exhibits retinoid receptor-independent apoptotic properties. Phase III clinical trial data has suggested that fenretinide reduces breast cancer relapse in pre-menopausal women. Fenretinide is the most studied retinoid in breast cancer chemoprevention clinical trials due to its selective accumulation in breast tissue and its favorable toxicological profile. This agent showed a significative reduction of the incidence of second breast tumors in premenopausal women confirmed after 15-year followups. Fenretinide, a drug being developed by Sirion Therapeutics, slowed the progression of advanced dry age-related macular degeneration (AMD) by 45 percent for people receiving a higher dose of the treatment in a Phase II clinical trial. Sirion has been granted a Fast Track designation for the treatment by the FDA. Fenretinide is in phase II clinical trials for the treatment of B-cell lymphoma, chronic lymphocytic leukemia. It is also in phase I clinical trials for the treatment of cystic fibrosis.
Status:
Other

Class (Stereo):
CHEMICAL (ACHIRAL)

Status:
Other

Class (Stereo):
CHEMICAL (ACHIRAL)

Status:
Other

Class (Stereo):
CHEMICAL (ACHIRAL)

Status:
Other

Class (Stereo):
CHEMICAL (ACHIRAL)

N-Methyl-DL-Aspartic Acid (NMDLA) represents a racemic mixture of D and L enantiomers (NMDA; NMLA). Each enantiomer has different biological activities and different natural tissue/species abundances. Therefore, each enantiomer should be considered separately. NMDA is a widely studied neurotoxin which is an agonist of the NMDA receptor and induces brain legions. NMDA is not normally found in tissues, while NMLA can be found naturally in some bivalves.

Showing 201 - 210 of 693 results