Bicalutamide
Bicalutamide. First-generation non-steroidal AR antagonist. Used in combined androgen blockade for prostate cancer; also off-label for transgender… Oral half-life 7 d.
First-generation non-steroidal AR antagonist. Used in combined androgen blockade for prostate cancer; also off-label for transgender hormone therapy as an antiandrogen with minimal endocrine side effects. CYP3A4 substrate.
PK: THE CITED PAPER CARRIES FOUR EXCELLENT VERBATIM NUMBERS AND NONE OF THEM WERE THE FOUR STORED — "Median T(max) was 24 hours for both formulations. The C(max) ... was 1176.2 (191.6) ... The corresponding values for AUC(0-672) were 277,503 (66,865) ... mug . h/L" at 50 mg — against which the stored record was 2.20x under on exposure, 2.32x under on peak and 1.90x late on the peak time. The values adopted are FITTED to reproduce all three of those verbatim measurements and are disclosed as fitted: no abstract states a bicalutamide volume or absorption rate at all, and F 1 is an assumption because this drug has no human intravenous form. MY WARFARIN-SHAPED PRIOR THAT ONE HALF-LIFE MUST BE A TWO-ENANTIOMER BLEND IS REFUTED, AND THE RECORD ALREADY DOCUMENTED WHY: the R-enantiomer peaks at 559-970 ng/mL and declines over 4.2 days while S peaks at 32-66 ng/mL and clears in 19 h, and "Plasma concentrations of the racemate were in very good agreement with the sum of the enantiomer concentrations" — so past the first day THE RACEMATE CURVE IS THE R CURVE. The half-life becomes the verbatim "a long plasma elimination half-life (1 week)". Its free fraction stays label-grade: the only indexed figure is "greater than 95%", an inequality that must not be entered as a point value.
Pharmacokinetics
- Oral — t½ 7.0 d · F 100% · ka 0.155 h⁻¹ · Vd 41 L
Sources: PMID:21353117, PMID:19359544, PMID:8310708, PMID:15509184