Pirmitegravir is a potent and first-in-class inhibitor of allosteric integrase ( ALLINI ) that targets LEDGF/p75 binding site. Pirmitegravir displays picomolar IC 50 in human PBMCs with a >24,000 therapeutic index against HIV-1. Pirmitegravir harbors outstanding anti-virus and safety properties.

Pirmitegravir (Compound STP0404) inhibits dual tropic HIV-189.6 at 1.4 nM IC 50 in CEMx174 cells[1]. Pirmitegravir (Compound STP0404) is a highly potent ALLINI with picomolar to single-digit nanomolar IC 50 values that inhibits both wild type and Ral-resistant HIV-1 strains[1]. Pirmitegravir (Compound STP0404) displays IC 50 of 0.41 nM against HIV-1NL4-3 without observable cytotoxicity in human PBMCs at 10 μM (TC 50 >10μM)[1].

Pirmitegravir (Compound STP0404) displays appropriate PK profiles for once daily administration[1]. Pirmitegravir (Compound STP0404) lacks micronucleus-inducing and bone marrow cell proliferation inhibitory potentials in rats (500, 1000 and 2000 mg/kg/day), supporting that STP0404 is not genotoxic[1]. Assessment of Pharmacokinetics (PK) profile of Pirmitegravir (Compound STP0404) in rat and dog[1]. PK Values Rat Dog 10 mg/kg (p.o) 5 mg/kg (i.v) 2 mg/kg (p.o) 2 mg/kg (i.v) T 1/2 (hr) 4.56 3.83 6.90 6.11 AUC (hr.nM) 78074 42676 4683 9260 C max (nM) 21380 - 3983 - F t (%) 92.8 - 50.6 - Animal Model: SD rats and beagle dogs[1]Dosage: 1, 2, 5, and 10 mg/kg Administration: i.v.; p.o. Result: The half-life (T1/2) was 3–7 h, and oral bioavailability (Ft) was 50–93% in these two animal species. Systemic exposure, which was determined by area under the curve and maximum concentration of STP0404 in plasma (AUC and C max ), increased dose-dependently from 2 to 10 mg/kg.

2245231-10-9

C27H31ClN4O3

495.01

Pirmitegravir

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years