Abiraterone Acetate/Niraparib

Preferred Label : Abiraterone Acetate/Niraparib;

NCIt synonyms : Niraparib/Abiraterone Acetate; Niraparib Tosylate Monohydrate/Abiraterone Acetate; Abiraterone Acetate and Niraparib Tosylate Monohydrate; Abiraterone Acetate/Niraparib Tosylate Monohydrate; Niraparib and Abiraterone Acetate; Niraparib Tosylate Monohydrate and Abiraterone Acetate;

NCIt definition : An orally bioavailable fixed dose combination agent containing the acetate ester prodrug of the steroidal compound abiraterone, an inhibitor of the cytochrome p450 (CYP) family member 17 alpha-hydroxylase/C17,20-lyase (CYP17; CYP17A1), and the tosylate monohydrate salt form of niraparib, an inhibitor of poly (ADP-ribose) polymerase (PARP) types 1 and 2 (PARP-1 and -2), with anti-androgen and antineoplastic activities. Upon administration of abiraterone acetate/niraparib, abiraterone acetate is converted to its active form abiraterone, which, in turn, targets, binds to and inhibits the enzymatic activity of CYP17, thereby preventing the formation of steroid intermediates and androgens involved in androgen synthesis. This suppresses testosterone production by testes, adrenals and testosterone-dependent prostate tumor cells in order to decrease testosterone to castrate-range levels, which inhibits proliferation of testosterone-dependent cancer cells. In addition, niraparib binds to and inhibits the activity of PARP-1 and -2, thereby inhibiting PARP-1 and -2-mediated DNA repair, enhancing the accumulation of DNA strand breaks, and promoting genomic instability, which results in cancer cell apoptosis. PARP family proteins are often overexpressed in cancer cells and are activated by single-strand DNA (ssDNA) breaks to catalyze post-translational ADP-ribosylation of nuclear proteins, which promotes DNA repair and cancer cell survival.;

Drug name : Akeega;

Molecule name : CJNJ-67652000;

NCI Metathesaurus CUI : CL1905133;

Origin ID

C191876;

UMLS CUI

C5784759;

Semantic type(s)
- Pharmacologic Substance [UMLS semantic type]
chemical_or_drug_affects_gene_product
- Poly [ADP-Ribose] Polymerase 1 [NCIt concept]
concept_is_in_subset
- CTRP Agent Terminology [NCIt concept]
- CTRP Terminology [NCIt concept]
- GDC Terminology [NCIt concept]
- GDC Therapeutic Agent Terminology [NCIt concept]
- NCI Drug Dictionary Terminology [NCIt concept]
- NCIt Antineoplastic Agent Terminology [NCIt concept]
has_target
- Poly [ADP-Ribose] Polymerase 1 [NCIt concept]
- Poly [ADP-Ribose] Polymerase 2 [NCIt concept]
- Steroid 17-Alpha-Hydroxylase/17,20 Lyase [NCIt concept]
is_component_of_chemotherapy_regimen
- Abiraterone/Niraparib/Prednisone Regimen [NCIt concept]

Keyword's position in hierarchy(ies) :

Details

Main resources

You can consult :