Tesamorelin

peptide · endocrine · Subcutaneous

Tesamorelin, a peptide. Full-length GHRH (1-44) conjugated with trans-3-hexenoic acid at the N-terminus — blocks DPP-IV degradation and… Subcutaneous half-life 0.1 h.

Full-length GHRH (1-44) conjugated with trans-3-hexenoic acid at the N-terminus — blocks DPP-IV degradation and extends plasma t½. FDA-approved for reducing visceral adipose tissue (VAT) in HIV-associated lipodystrophy. Durable GH-pulse restoration with preserved pituitary negative feedback.

PK: Gonzalez-Sales 2015 (PMID:25358450), 38 HIV-infected patients and healthy subjects, SC 1-2 mg daily for 14 days, verbatim "Volume of distribution was calculated to be 200 L (17.7 %)" and "Plasma clearance ... 1,060 L/h (33.6 %)". The half-life is that fit's own ln2 x V/CL = 0.13 h, which is where the stored value came from — but the record had kept the derived half-life while storing V as 7 L, a registry default, so the set contradicted itself. V is restored to the paper's 200 L and F pinned to 1, since both parameters are apparent after SC-only dosing. ka 2 /h and F 0.04 dropped: neither is stated anywhere. The nearest half-life in any other source is 26 min in DOG (PMID:15113616), and that paper's 13% is an INHALED bioavailability, not subcutaneous.

Pharmacokinetics

Sources: PMID:21668043