Cinacalcet
Cinacalcet. Calcimimetic — positive allosteric modulator of the calcium-sensing receptor (CaSR) in parathyroid chief cells → decreased PTH… Oral half-life 30 h.
Calcimimetic — positive allosteric modulator of the calcium-sensing receptor (CaSR) in parathyroid chief cells → decreased PTH secretion. Used for secondary hyperparathyroidism in CKD-on-dialysis + parathyroid carcinoma.
PK: F 0.225 is the EXACT MIDPOINT of "poor oral bioavailability of 20 to 25%" — and that sentence is a BACKGROUND CLAIM in a NANOPARTICLE FORMULATION-DEVELOPMENT paper WHOSE SPECIES IS NEVER STATED, whose own result is merely a relative doubling against an aqueous suspension. Half-life 35 h is likewise the exact midpoint of a stated "30-40 hours"; the lower endpoint is now carried. NO CINACALCET VOLUME EXISTS IN ANY ABSTRACT — a search returns zero records — and there is no intravenous formulation, so the 1000 L is necessarily APPARENT; F is pinned to 1, which removes a double-division that had been inflating the effective volume to about 4400 L. The volume itself is retained as an unsourced label figure rather than deleted, because the resolver default would be twenty-fold too small for this drug. ka 0.3 dropped. Effect broadly tracks plasma: parathyroid hormone nadir at 2-3 h against a 2-6 h time to peak.
Pharmacokinetics
- Oral — t½ 30 h · F 100% · Vd 1000 L
Sources: PMID:32486863, PMID:19566113