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AMX12006 is a potent, selective and orally active EP4 antagonist with an IC50 value of 4.3 nM. AMX12006 shows cytotoxic and antitumor activity[1]. | [in vivo]
AMX12006 (75, 150 mg/kg; p.o.; once daily for 11 days) shows antitumor activity in a dose-dependent manner[1].
Pharmacokinetic Parameters of AMX12006 in Sprague-Dawley rats[1].
| iv, 1 mg/kg | po, 10 mg/kg | | Tmax (h) | | 0.5 | | Cmax (ng/mL) | 4627 ± 304 | 8243 ± 370 | | AUC(0-t)(h·ng/mL) | 3375 ± 477 | 25672 ± 5668 | | AUC0–∞ (h·ng/mL) | 3416 ± 495 | 25707 ± 5682 | | T1/2(h) | 1.4 ± 0.3 | 2.7 ± 0.2 | | CL (mL/min/kg) | 4.95 ± 0.77 | | | Vdss (L/kg) | 0.41 ± 0.04 | | | F % | | 76.1 |
Sprague-Dawley rats, 1 mg/kg iv ; 10 mg/kg po [1] | [IC 50]
hEP4: 4.3 nM (IC50) | [References]
[1] Debasis Das, et al. Discovery of Novel, Selective Prostaglandin EP4 Receptor Antagonists with Efficacy in Cancer Models. ACS Med. Chem. Lett. 2023. |
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