Etravirine is a non-nucleoside reverse transcriptase inhibitor (NNRTI) and active pharmaceutical ingredient (API) used in antiretroviral therapy for the treatment of HIV-1 infection. It is generally used in combination with other antiretroviral medicines, particularly in patients with HIV-1 strains that have resistance to other NNRTIs.
Etravirine is a diarylpyrimidine-derived NNRTI that inhibits HIV-1 reverse transcriptase. By binding to a site distinct from the enzyme's active site, it interferes with viral DNA synthesis and inhibits HIV replication.
CAS Number: 269055-15-4
Molecular Formula: C₂₀H₁₅BrN₆O
Molecular Weight: 435.28 g/mol
Etravirine binds to HIV-1 reverse transcriptase at an allosteric site and inhibits the enzyme's ability to convert viral RNA into DNA.
Its antiviral effects include:
Etravirine is used in pharmaceutical formulations for:
The exact therapeutic application depends on the formulation, patient population, country and applicable regulatory labeling.
Etravirine is a synthetic antiretroviral API with defined chemical and physicochemical characteristics. Pharmaceutical-grade material requires appropriate control of identity, assay, related substances, stereochemical purity and other quality attributes.
Typical quality evaluation may include:
Pharmaceutical-grade Etravirine should comply with the applicable approved specification, pharmacopoeial requirements where applicable, and relevant regulatory standards.
A qualified supplier should provide Certificate of Analysis (CoA), specification sheet, SDS/MSDS, batch traceability and applicable regulatory documentation.
Store Etravirine in a tightly closed container, protected from excessive moisture, heat and direct light, according to the manufacturer's approved storage and stability requirements.
| Parameter | Specification |
|---|---|
| Appearance | White to off-white crystalline powder |
| Identification | IR & HPLC compliant |
| Assay (HPLC) | NLT 98.0% by HPLC |
| Loss on Drying | NMT 1.0% |
| Residue on Ignition | NMT 0.2% |
| Heavy Metals | NMT 10 ppm |
| pH (1% Solution) | 2.0 – 4.0 |
| Individual Impurity | ≤ 0.5% |
| Total Impurities | ≤ 1.5% |
| Water Content | NMT 0.5% |