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Rilpivirine hydrochloride

Cat. No. M30512
Rilpivirine hydrochloride Structure
Synonym:

TMC-278 hydrochloride; TMC278 hydrochloride; TMC 278 hydrochloride

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Quality Control & Documentation
Biological Activity

Rilpivirine (R278474) hydrochloride is a potent and specific diarylpyrimidine (DAPY) non-nucleoside reverse transcriptase inhibitor (NNRTI). Rilpivirine hydrochloride has high antiviral activity against wild-type HIV (EC50=0.4 nM) and mutant viruses (EC50=0.1-2.0 nM). Rilpivirine hydrochloride has a high genetic barrier to resistance development of HIV.

Chemical Information
Molecular Weight 402.88
Formula C22H19ClN6
CAS Number 700361-47-3
Storage Please store the product under the recommended conditions in the Certificate of Analysis.
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Elahe Taki, et al. Expert Rev Anti Infect Ther. Cabotegravir/Rilpivirine: the last FDA-approved drug to treat HIV

[2] Daryl Hodge, et al. Clin Pharmacokinet. Pharmacokinetics and Drug-Drug Interactions of Long-Acting Intramuscular Cabotegravir and Rilpivirine

[3] Edgar T Overton, et al. Lancet. Long-acting cabotegravir and rilpivirine dosed every 2 months in adults with HIV-1 infection (ATLAS-2M), 48-week results: a randomised, multicentre, open-label, phase 3b, non-inferiority study

[4] A Markham. Drugs. Cabotegravir Plus Rilpivirine: First Approval

[5] Susan Swindells, et al. N Engl J Med. Long-Acting Cabotegravir and Rilpivirine for Maintenance of HIV-1 Suppression

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Keywords: Rilpivirine hydrochloride, TMC-278 hydrochloride; TMC278 hydrochloride; TMC 278 hydrochloride supplier, Anti-infection, inhibitors, activators


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