Summary of Use during Lactation

Etravirine is excreted in breastmilk in concentrations exceeding the maternal plasma and appears to increase in concentration over time. Until more information becomes available, an alternate agent may be preferred. Achieving and maintaining viral suppression with antiretroviral therapy decreases breastfeeding transmission risk to less than 1%, but not zero. Individuals with HIV who are on antiretroviral therapy with a sustained undetectable viral load and who choose to breastfeed should be supported in this decision. If a viral load is not suppressed, banked pasteurized donor milk or formula is recommended.[1,2]

Drug Levels

Maternal Levels. Nine HIV-positive women had etravirine added to their existing antiretroviral regimens between postpartum days 1 and 14 postpartum. The dosage was not stated, but was presumably 200 mg twice daily. Breastmilk and maternal serum samples were obtained at 0, 2, 5, 8 and 24 hours after the dose of etravirine on days 5 and 14 postpartum. The median breastmilk concentration of etravirine on day 5 was 241 mcg/L (range 161 to 891 mcg/L) and on day 14 was 798 mcg/L (range 161 to 2714 mcg/L). The median milk to plasma ratio was 1.09 on day 5 and 3.27 on day 14.[3]

Infant Levels. Relevant published information was not found as of the revision date.

Effects in Breastfed Infants

Relevant published information was not found as of the revision date.

Effects on Lactation and Breastmilk

Relevant published information was not found as of the revision date.

Alternate Drugs to Consider

Lamivudine, Nelfinavir, Nevirapine, Zidovudine

References

1.

World Health Organization. Consolidated guidelines on HIV prevention, testing, treatment, service delivery and monitoring: recommendations for a public health approach. 2021. https://www​.who.int/publications​/i/item/9789240031593 [PubMed: 34370423]

2.

Department of Health and Human Services. Recommendations for the use of antiretroviral drugs during pregnancy and interventions to reduce perinatal HIV transmission in the United States. Infant feeding for individuals with HIV in the United States. 2023. https:​//clinicalinfohivgov​/en/guidelines​/perinatal/infant-feeding-individuals-hiv-united-states?view=full

3.

Spencer LY, Liu S, Wang CH, et al. Intensive etravirine PK and HIV-1 viral load in breast milk and plasma in HIV+ women receiving HAART. Topics Antiviral Med 2014;22:466. https://www​.iasusa.org/tam/april-2014

Substance Name

Etravirine

CAS Registry Number

269055-15-4

Drug Class

Breast Feeding

Lactation

Milk, Human

Anti-Infective Agents

Antiviral Agents

Anti-HIV Agents

Anti-Retroviral Agents

Reverse Transcriptase Inhibitors