BMS-707035

BMS-707035 is a potent orally active HIV-1 integrase strand transfer inhibitor (INSTI). BMS-707035 has enzyme inhibitory with an IC₅₀ value of 3 nM. BMS-707035 also has weak CYP inhibiton and antiviral activity. BMS-707035 can be used for the research of human immunodeficiency virus-1 (HIV-1)^[1]. In Vitro: BMS-707035 has antiviral activity with EC₅₀ values of 2 nM and 17 nM in the presence of 10% FBS and 15 mg/mL human serum albumin, respectively^[1].
BMS-707035 has high plasma protein binding and not overtly cytotoxicy to several cell lines, with CC₅₀ value of ≥45 μM^[1].
BMS-707035 has a relatively weak CYP inhibiton with IC₅₀ value of ≥40 μM^[1]. In Vivo: BMS-707035 has a low clearance effect in the rat, dog and monkey with moderate to long elimination half-lives in all species^[1].
Pharmacokinetic Parameters of BMS-707035 in rat, dog and monkey (IV)^[1].

	Rat	Monkey	Dog
IV dose (mg/kg)	0.87	1	1
CL (ml/min/kg)	9.7	6.8	2.0
T1/2(h)	4.0	6.5	6.0
Vss(L/kg)	0.86	0.87	0.45
PO dose (mg/kg)	4.4	5	5.2
Cmax(μM)	4.51	6.12	72.8
tmax(h)	0.25	0.25	0.25
AUC (μM*h)	19.1	19.2	162
F (%)	86	56	129