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) |
| T1/2 (hr) | 4.56 | 3.83 | 6.90 | 6.11 |
| AUC (hr.nM) | 78074 | 42676 | 4683 | 9260 |
| Cmax (nM) | 21380 | - | 3983 | - |
| Ft (%) | 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 Cmax), increased dose-dependently from 2 to 10 mg/kg. |
![1H-Pyrrolo[2,3-b]pyridine-5-acetic acid, 4-(4-chlorophenyl)-α-(1,1-dimethylethoxy)-2,3,6-trimethyl-1-[(1-methyl-1H-pyrazol-4-yl)methyl]-, (αS)- Structure](/CAS/20211123/GIF/2245231-10-9.gif)