Abiraterone
Abiraterone. CYP17A1 (17α-hydroxylase / C17,20-lyase) inhibitor — blocks androgen biosynthesis in testes, adrenals, and prostate tumor cells. Used with prednisone to…
CYP17A1 (17α-hydroxylase / C17,20-lyase) inhibitor — blocks androgen biosynthesis in testes, adrenals, and prostate tumor cells. Used with prednisone to mitigate compensatory mineralocorticoid excess from upstream pregnenolone accumulation. Castration-resistant prostate cancer.
PK REMOVED. ITS CITATION CHARACTERISES THE PRODRUG ITS OWN ABSTRACT CALLS UNDETECTABLE — every quoted parameter, including "The apparent elimination half-life (t1/2) showed a mean of 8.98 +/- 3.92 h", belongs to abiraterone ACETATE. The stored t-half 14 is verbatim nowhere. F 0.1 IS AN INEQUALITY BOUND, "poor oral bioavailability (<10%) and a dramatic positive food effect (5-10-fold)", with a second candidate in the cited abstract itself, an assay limit of "0.1 ng/ml for abiraterone". AND A SCALAR F IS INDEFENSIBLE: fed-versus-fasted AUC is "351.64%" and Cmax "478.45%", and dosing around meals moves exposure "by 57 %, 595 %, and 649 %". V 19000 is the label figure; the only published human volumes are explicitly apparent, "large apparent central (5,620 L) and peripheral (17,400 L) volumes", and pairing an apparent volume with F 0.1 discounted tenfold twice. Absorption is not first-order at all — it needs "an Erlang-type absorption model ... with three-transit compartments". mw 349.51 IS CORRECT and untouched: it is the free base, the circulating species.
Sources: PMID:30671920, PMID:25204404, PMID:31981706, PMID:37574850, PMID:25344090