Table 1.

Physicochemical properties, in vitro and population pharmacokinetic data of anti-TB drugs

	Bedaquiline	Delamanid	Isoniazid	Rifapentine
log Po:w	6.37 28	5.53 29	−0.7 30	4.0 31
pKa	13.61, 8.91 28	3.99 29	1.82 30	7.17, 7.01 31
Blood-to-plasma ratio	*4.04	*3.92	*0.80	0.56 32
Protein binding (%)	99.9 28	99.55 33	10 30	97.7 31
Plasma clearance	0.04 ± 0.002 34	0.729 ± 0.121 15	‡0.142 ± 0.042 35	0.028 ± 0.009 17
Absorption rate (h−1)	1.03 ± 0.19 36	§0.96 37	2.28 35	#0.42 37
Vd (L/kg)	2.18 34	7.32 15	0.21 38	0.69 17
Bioavailability (%)	∆10034	36 (25-47) 15	∆10035	φ45 (40-50)39

log P_o:w – Partition coefficient between octanol and water; pKa – logarithmic value of the dissociation constant; V_d – volume of distribution;

^*blood-to-plasma ratios were computed using equations from Paixão et al.⁴⁰;

^†Computed from the PBPK model; Plasma clearance values are given for adults and are represented as L/h/kg,

^‡Value provided is apparent clearance of slow acetylators,

^§Computed from polar surface area and hydrogen bond donor values using the equation from Gertz et al.⁴¹,

^#Computed from Caco-2 permeability using the equation from Gertz et al.⁴¹,

^∆Bioavailability has been fixed to 100 in the population pharmacokinetic studies.

^φA bioavailabity between 40-50% was assumed based on the relative bioavailility of 70% for the oral formulation compared to oral formulation