HIV-1 protease-IN-7 (compound 16) is an orally active HIV-1 protease inhibitor (IC50=3.52 nM, EC50=37 nM)[1].
in vivo
HIV-1 protease-IN-7 (2.57 mg/kg; p.o.; single) exhibits good plasma total clearance and oral bioavailability[1].
Animal Model:
Male Sprague-Dawley rats (8-week-old)[1].
Dosage:
2.57 mg/kg (2 μM/kg)
Administration:
Oral administration; single.
Result:
1.19Pharmacokinetic Parameters of HIV-1 protease-IN-7 in male Sprague-Dawley rats[1].
metabolic stability rat/human (%)
CLtot (mL/min/kg)
Vdss (L/kg)
t1/2 (h)
F (%)
serum fu(%)
PO (2.57 mg/kg)
63/23
8.2
1.9
3.9
3.3
0.1
References
[1] Kusumoto Y, et al. Highly Potent and Oral Macrocyclic Peptides as a HIV-1 Protease Inhibitor: mRNA Display-Derived Hit-to-Lead Optimization. ACS Medicinal Chemistry Letters, 2022.
