Efavirenz
Also known as: Sustiva, Stocrin, Efavir, Estiva (component of Atripla, Trustiva, TLE regimens)
CAS Number: 154598-52-4
Non-Nucleoside Reverse Transcriptase Inhibitor (NNRTI)
Pharmacopeia Standards
Mechanism of Action
Efavirenz is a benzoxazinone that binds a hydrophobic allosteric pocket on the p66 subunit of HIV-1 reverse transcriptase, adjacent to but distinct from the catalytic site. Binding locks the enzyme in a conformation that greatly slows the chemical step of polymerisation, producing non-competitive inhibition of both RNA-dependent and DNA-dependent DNA polymerase activity. It has no meaningful activity against HIV-2 or host DNA polymerases.
Technical Specifications
| Generic / INN Name | Efavirenz |
| CAS Registry Number | 154598-52-4 |
| Molecular Formula | C14H9ClF3NO2 |
| Molecular Weight | 315.67 g/mol g/mol |
| Typical Purity | Not less than 98.0% on anhydrous basis; enantiomeric purity not less than 99.5% |
| Storage Conditions | Store below 25 degrees C in tightly closed HDPE drums with LDPE liners, protected from light and moisture. |
| Shelf Life | 48 months from date of manufacture in original sealed packing |
| Category | Antiretrovirals (HIV) |
Specifications are indicative and intended for sourcing reference only. Always confirm against the supplier's Certificate of Analysis and the applicable pharmacopeial monograph before issuing a purchase specification.
Typical Applications
Bulk API for 400 mg and 600 mg tablets and for tenofovir-lamivudine-efavirenz and tenofovir-emtricitabine-efavirenz fixed-dose combinations, plus paediatric capsules and sprinkle formulations.
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