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Vulolisib is a potent and orally active phosphatidylinositol 3-kinase (PI3K) inhibitor, with IC50 values of 0.2 nM, 168 nM, 90 nM and 49 nM for PI3Kα, PI3Kβ, PI3Kγ and PI3Kδ, respectively. Antiproliferative and antineoplastic activity[1]. | [in vivo]
Vulolisib (10, 30 and 60 mg/kg; IG; daily for 7days) exhibits better tolerance and exposure than Inavolisib[1].
Vulolisib (10mg/kg; PO; daily for 19 days) inhibits tumor growth with TGI of 132%[1].
Vulolisib (5 mg/kg; IG, single dosage) exhibits favorable pharmacokinetic property[1].
Pharmacokinetic Parameters of Vulolisib in male Balb/c mice[1].
| IG (5 mg/kg) | | tmax (h) | 0.5 | | Cmax (ng/mL) | 1057 | | AUC0-t (ng/mL·h) | 2185 | | AUC0-∞ (ng/mL·h) | 2274 | | t1/2 (h) | 1.6 | | MRT (h) | 2.2 |
| Animal Model: | Sprague-Dawley rats[1] | | Dosage: | 10, 30 and 60 mg/kg | | Administration: | IG; daily for 7days | | Result: | Exhibited better tolerance and exposure than Inavolisib. |
| Animal Model: | Female BALB/c nude mice (6-8 weeks; injected with HCC1954)[1] | | Dosage: | 10mg/kg | | Administration: | PO; daily for 19 days | | Result: | Inhibited tumor growth with TGI of 132%. |
| Animal Model: | Male Balb/c mice[1] | | Dosage: | 5 mg/kg | | Administration: | IG, single dosage (Pharmacokinetic Analysis) | | Result: | Exhibited favorable pharmacokinetic property. |
| [IC 50]
PI3Kα: 0.2 nM (IC50); PI3Kβ: 168 nM (IC50); PI3Kγ: 90 nM (IC50); PI3Kδ: 49 nM (IC50) | [References]
[1] Xiaolan ZHAN, et al. Three fused ring derivative-containing salt or crystal form and pharmaceutical composition thereof. WO2021104146A1 (example 22) |
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