Table 4.

In Vitro ADME Profiles for AZM, 22, and 26

Comp	LogPa	Solubility (μM)b	Papp A → Bc	Papp B → Ac	HLM % remainingd	Half-life (min)
AZM	−0.86	3200e	0.19f	0.77f	-	-
22	1.49	32.8	6.5	14.1	62	74
26	−1.54	126.6	< 0.17g	<0.17g	86	297

^aCalculated using pKCSM.⁷¹

^bSolubility in PBS at pH 7.4 at equilibrium at room temperature at 24 hr.

^cBi-directional Caco-2 permeability with pH 6.5/7.4 for donor/receiver chambers, respectively. A = apical, B = basolateral. P_app is the apparent permeability coefficient (10⁻⁶ cm/sec).

^dHLM = human liver microsomes. Tested at 37 °C in 0.1 mg/mL HLMs. % remaining is percentage of comopound remaining in sample at 60 min time point and is average of 2 replicates.

^eGranero et al.⁴⁵ measured in water at 25 °C.

^fCrowe et al.⁴⁶ measured at pH 6.0/7.4 in donor/receiver chambers.

^gDetection was below limit of quantitation in receiver sample.