Summary of Use during Lactation

Limited information indicates that maternal rilpivirine doses of 25 mg daily produce low levels in milk and infant serum. Until more data become available, an alternate drug may be preferred, especially while nursing a newborn or preterm infant. 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] Extended postnatal prophylaxis of breastfed infants with rilpivirine should continue until breastfeeding is stopped.[3]

Drug Levels

Maternal Levels. Two mothers taking rilpivirine 25 mg once daily provided milk samples at a median of 15.5 hours after a dose. The median drug concentration in milk was 123 mcg/L, which resulted in an estimated infant dosage of 20 mcg/kg daily.[4]

In a retrospective study in a German hospital of mothers who were receiving antiretroviral prophylaxis, 3 mothers were receiving rilpivirine 25 mg once daily. Breastmilk levels obtained at unspecified times with respect to the dose at 1, 4, and 6 months postpartum were mostly <50 mcg/L in two of the patients. In the third mother, the milk level was 4300 mcg/L at 4 months after which breastfeeding was discontinued.[5]

Infant Levels. An infant was breastfed by a mother taking rilpivirine 25 mg once daily, although the extent of breastfeeding was not sated. The infant’s serum concentrations taken 16 hours after maternal drug intake at 1 month of age was 4 mcg/L.[4]

In a retrospective study in a German hospital of mothers who were receiving rilpivirine 25 mg once daily, three exclusively breastfed their infants. Infant serum concentrations obtained at unspecified times in two of the infants was <50 mcg/L at 1 and 4 months of age. In the third infant whose mother had high rilpivirine milk levels, the infant serum level was 660 mcg/L at 1 month and 10,450 mcg/L at 4 months of age, at which time breastfeeding was discontinued.[5]

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.

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. 2024 https:​//clinicalinfo​.hiv.gov/sites/default​/files/guidelines/documents​/perinatal-hiv​/guidelines-perinatal.pdf

3.

Van de Perre P, Moles JP, Nagot N. HIV postnatal prophylaxis: How long is long enough? Expert Rev Anti Infect Ther 2025;23:1075–81. [PubMed: 41216942]

4.

Aebi-Popp K, Kahlert CR, Crisinel PA, et al. Transfer of antiretroviral drugs into breastmilk: A prospective study from the Swiss Mother and Child HIV Cohort Study. J Antimicrob Chemother 2022;77:3436–42. [PMC free article: PMC9704434] [PubMed: 36177836]

5.

Spielberger BD, Zink A, Rohr JC, et al. Breastfeeding on ART and a closer look at drug transfer to HIV-exposed uninfected infants. Sci Rep 2025;15:32612. [PMC free article: PMC12446422] [PubMed: 40968165]

Substance Name

Rilpivirine

CAS Registry Number

500287-72-9

Drug Class

Breast Feeding

Lactation

Milk, Human

Anti-Infective Agents

Antiviral Agents

Anti-HIV Agents

Anti-Retroviral Agents

Reverse Transcriptase Inhibitors