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. Author manuscript; available in PMC: 2021 May 28.
Published in final edited form as: J Med Chem. 2020 May 6;63(10):5501–5525. doi: 10.1021/acs.jmedchem.0c00442

Table 6.

Pharmacokinetic characterization of 13a with iv and oral administration.

13a 13a Panobinostat93
Administered dose (mg/kg) iv at 5 mg/kg oral at 20 mg/kg oral at 50 mg/kg
Cmax (ng/mL) -- 45.1 116
t1/2 (h) 15.2 7.45 2.9
AUC0-inf (ng·h/mL) 334 265 126
F% -- 19.8 4.62
a

13a was injected via iv and oral (n = 3), blood was sampled at different time-points after dosing for 24 h, and the inhibitor plasma concentration is determined via LC-MS/MS. The area under the plasma concentration versus time curve (AUC) is calculated using the linear trapezoidal method. The PK data are fitted to obtain PK parameters using the non-compartmental method.