Rilpivirine HCl (Rilpivirine hydrochloride) is a selective and potent non-nucleoside reverse transcriptase inhibitor (NNRTI) with antiviral activity that inhibits the HIV virus and can be used in the study of HIV infections.

HIV-1 (wild-type):EC50=0.4 nM

Rilpivirine HCl showed significant activity against wild-type HIV-1 (EC50=0.4 nM) and activity ranged from EC50=0.1-2.0 nM against all single and double mutants tested. no indication of breakthrough of wild-type HIV-1 at 1 μM was observed with Rilpivirine HCl in 30-day experiments at concentrations ranging from 10 to 5000 nM. Rilpivirine HCl was able to inhibit 81% of clinical isolates (approximately 1,200 recombinant clinical isolates) with an EC50 of less than 1 nM and 94% of clinical isolates with an EC50 of less than 10 nM. [1]
Rilpivirine HCl showed sub-nanomolar activity against HIV-1 Group M wild-type isolates with EC50s ranging from 0.07 to 1.01 nM. [2]

Oral administration of Rilpivirine HCl in rats (10-160 mg/kg for 1 month) did not elicit significant abnormal responses, except for increased liver weight and species-specific thyroid hypertrophy observed at some of the higher doses.
The elimination half-life of intravenously administered Rilpivirine HCl ranged from 4.4 hours in rats to 31 hours in dogs, with drug exposures (AUCinf) ranging from 3.1 μg-h/mL in rats (4 mg/kg), to 8.7 μg-h/mL in dogs (1.25 mg/kg), 1.4 μg-h/mL in monkeys (1.25 mg/kg), and 1.4 μg-h/mL in rabbits ( 1.25 mg/kg) and 44 μg-h/mL in rabbit (1.25 mg/kg).
When administered orally, the half-life of Rilpivirine HCl was 2.8 hours in rats and 39 hours in dogs, with oral bioavailability of 32% and 31% in rats and dogs, respectively. [1]