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Recommendations for Use of Antiretroviral Drugs in Pregnant HIV-1-Infected Women for Maternal Health and Interventions to Reduce Perinatal HIV Transmission in the United States

Non-Nucleoside Reverse Transcriptase Inhibitors

Rilpivirine (Edurant, RPV)

(Last updated: August 6, 2015; last reviewed: August 6, 2015)

Rilpivirine is classified as Food and Drug Administration Pregnancy Category B.

Animal Studies

Rilpivirine was neither mutagenic nor clastogenic in a series of in vitro and animal in vivo screening tests. Rilpivirine was not carcinogenic in rats when administered at doses 3 times higher than exposure in humans at the recommended dose of 25 mg once daily. Hepatocellular neoplasms were observed in both male and female mice at doses 21 times that of human therapeutic exposure; the observed hepatocellular findings in mice may be rodent-specific.

No effect on fertility was observed when rilpivirine was tested in rats at maternal doses up to 400 mg/kg/day, resulting in systemic drug exposure equivalent to 40 times the recommended human dose.

Teratogenicity/Developmental Toxicity
No evidence of embryonic or fetal toxicity or an effect on reproductive function was observed in rat and rabbit dams treated with rilpivirine during pregnancy and lactation at doses 15 and 70 times higher, respectively, than exposure in humans at the recommended dose of 25 mg once daily.

Placental and Breast Milk Passage 
Studies in lactating rats and their offspring indicate that rilpivirine is present in rat milk.

Human Studies in Pregnancy

A report describing rilpivirine pharmacokinetic (PK) evaluations at 32 weeks’ gestation and again postpartum in 2 HIV-infected pregnant women has been published. Rilpivirine area under the curve [AUC] was decreased by 30% to 43% during pregnancy. Postpartum AUC was similar to those seen in non-pregnant adults.2 An abstract presented PK and safety data from 32 HIV-infected pregnant women receiving rilpivirine. Median rilpivirine AUC and trough concentrations were reduced by about 20% in the second trimester and 30% in the third trimester, compared with postpartum.

Placental and Breast Milk Passage
In one published case report, cord blood and maternal plasma rilpivirine concentrations were 0.016 and 0.021 mg/L, for a cord blood/maternal concentration ratio of 0.74.2 An abstract has been presented including rilpivirine delivery concentration data from 9 mother-infant pairs, with median (range) cord blood rilpivirine plasma concentration of 53.8 ng/mL (<10.0 to 219.7 ng/mL), maternal delivery plasma rilpivirine concentration of 103.3 ng/mL (<10.0 to 273.4 ng/mL) and cord blood/maternal plasma ratio of 0.55 (0.38 to 0.83).3 No data exist on whether rilpivirine is excreted in breast milk in humans. 

Teratogenicity/Developmental Toxicity
The number of first-trimester exposures to rilpivirine that have been monitored to date in the Antiretroviral Pregnancy Registry is insufficient to allow conclusions to be drawn regarding risk of birth defects.4

Other Safety Data

No safety issues have been observed in the case report and the small PK study of rilpivirine in pregnancy.2,3 

Excerpt from Table 7a
Generic Name
Trade Name
Formulation Dosing Recommendations Use in Pregnancy

RPV (Endurant)
  • 25 mg
  • RPV 25 mg plus TDF 300 mg plus FTC 200 mg tablet
Standard Adult Dose
RPV (Endurant):
  • 25 mg once daily with food
  • 1 tablet once daily with food
PK in Pregnancy
  • RPV AUC and trough concentration reduced 20% to 30% in pregnancy compared with postpartum, but nearly all pregnant women exceeded target exposure.
Dosing in Pregnancy:
  • No dosing adjustment is needed for RPV during pregnancy.
Moderate to high placental transfer to fetus.b

No evidence of teratogenicity in rats or rabbits. Insufficient data to assess for teratogenicity in humans.
a Individual antiretroviral drug dosages may need to be adjusted in renal or hepatic insufficiency (for details, see Adult Guidelines, Appendix B, Table 7).
b Placental transfer categories—Mean or median cord blood/maternal delivery plasma drug ratio:
   High: >0.6
   Moderate: 0.3–0.6
   Low: <0.3

Key to Abbreviations: AUC = area under the curve; FTC = emtricitabine; PK = pharmacokinetic; RPV = rilpivirine; TDF = tenofovir disoproxil fumarate


  1. Rilpivirine [package insert]. Food and Drug Administration. 2013. Available at Accessed June 3, 2015.
  2. Colbers A, Gingelmaier A, van der Ende M, Rijnders B, Burger D. Pharmacokinetics, safety and transplacental passage of rilpivirine in pregnancy: two cases. AIDS. 2014;28(2):288-290. Available at
  3. Mirochnick M, Stek A, Kreitchman R, et al. Pharmacokinetics of Rilpivirine in HIV-Infected Women during Pregnancy and Postpartum. Presented at: 22nd Conference on Retroviruses and Opportunistic Infections. 2015. Seattle, WA.
  4. Antiretroviral Pregnancy Registry Steering Committee. Antiretroviral Pregnancy Registry international interim report for 1 Jan 1989–31 July 2014. Wilmington, NC: Registry Coordinating Center. 2014. Available at

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