Capsid Inhibitors
Lenacapavir (LEN)
Summary
- Pharmacokinetic data are insufficient to make dosing recommendations for oral or long-acting injectable lenacapavir (LEN) during pregnancy or breastfeeding.
- Clinical data are insufficient to characterize the risk for congenital anomalies associated with in utero exposure to LEN. No reproductive toxicity or teratogenicity concerns were identified in animal studies.
Human Studies in Pregnancy
Pharmacokinetics
No data are available on the pharmacokinetics (PK) of LEN with continuing subcutaneous injections during pregnancy.
Placental and Breast Milk Passage
No data are available regarding placental transfer of LEN. Additionally, no data are available describing breast milk passage of LEN in humans; because LEN is more than 98.5% protein bound, amounts found in breast milk are likely low.1
Teratogenicity/Adverse Pregnancy Outcomes
The Antiretroviral Pregnancy Registry has not monitored sufficient numbers of first-trimester exposures to LEN to report on the risk of overall birth defects.
Animal Studies
Carcinogenicity
LEN was not mutagenic in a series of in vitro and animal in vivo genotoxic assays; LEN was not carcinogenic in a mouse model.2
Reproduction/Fertility
In rats, no effects on fertility, mating performance, or early embryonic development were observed at LEN exposures 5 times greater than the exposure in humans at recommended doses.2
Teratogenicity/Adverse Pregnancy Outcomes
No significant toxicological effects on embryo-fetal development in rats and rabbits or pre- and postnatal development in rats were observed at area under the curve drug exposures approximately 16 times (rats) and 39 times (rabbits) the exposure in humans at recommended doses.2
Placental and Breast Milk Passage
LEN was detected at low levels in the plasma of nursing rat pups.2
Excerpt from Table 14
Generic Name (Abbreviation) Trade Name | Formulation | Dosing Recommendationsa | Use in Pregnancy |
---|---|---|---|
Lenacapavir (LEN) Sunlenca | LEN (Sunlenca)
| Pregnancy
Dosing in Pregnancy
Standard Adult Doses
Initiation Option 2
Maintenance Dosing
| No human data are available regarding placental passage or through breast milk. Data are insufficient to assess for teratogenicity in humans. No evidence of teratogenicity in rats or rabbits. |
a Individual ARV drug doses may need to be adjusted in patients with renal or hepatic insufficiency (for details, see the Adult and Adolescent Antiretroviral Guidelines, Appendix B, Table 12). Key: ARV = antiretroviral; LEN = lenacapavir; PK = pharmacokinetic; SQ = subcutaneous |
References
- National Institute of Child Health and Human Development. Lenacapavir. Drugs and Lactation Database (LactMed(R)). 2023. Available at: https://pubmed.ncbi.nlm.nih.gov/36701515.
- Sunlenca (lenacapavir) package insert [package insert]. Food and Drug Administration. 2022. Available at: https://www.accessdata.fda.gov/drugsatfda_docs/label/2022/215973s000lbl.pdf.
Capsid Inhibitors
Lenacapavir (LEN)
Excerpt from Table 14
Generic Name (Abbreviation) Trade Name | Formulation | Dosing Recommendationsa | Use in Pregnancy |
---|---|---|---|
Lenacapavir (LEN) Sunlenca | LEN (Sunlenca)
| Pregnancy
Dosing in Pregnancy
Standard Adult Doses
Initiation Option 2
Maintenance Dosing
| No human data are available regarding placental passage or through breast milk. Data are insufficient to assess for teratogenicity in humans. No evidence of teratogenicity in rats or rabbits. |
a Individual ARV drug doses may need to be adjusted in patients with renal or hepatic insufficiency (for details, see the Adult and Adolescent Antiretroviral Guidelines, Appendix B, Table 12). Key: ARV = antiretroviral; LEN = lenacapavir; PK = pharmacokinetic; SQ = subcutaneous |
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