Bictegravir use while Breastfeeding

Summary of Use during Lactation

Limited information indicates that maternal bictegravir 50 mg once 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.

Drug Levels

Maternal Levels. Three mothers taking bictegravir 50 mg once daily provided milk samples at a median of 8.5 hours after a dose. The median drug concentration in milk was 57 mcg/L, which resulted in an estimated infant dosage of 10 mcg/kg daily.[1]

Infant Levels. An infant was breastfed by a mother taking bictegravir 50 mg once daily, although the extent of breastfeeding was not sated. The infant’s serum concentrations taken 19 hours after maternal drug intake at 1 month of age was 103 mcg/L.[1]

Effects in Breastfed Infants

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

Effects on Lactation and Breastmilk

Gynecomastia has been reported among men receiving highly active antiretroviral therapy. Gynecomastia is unilateral initially, but progresses to bilateral in about half of cases. No alterations in serum prolactin were noted and spontaneous resolution usually occurred within one year, even with continuation of the regimen.[2-4] Some case reports and in vitro studies have suggested that protease inhibitors might cause hyperprolactinemia and galactorrhea in some male patients,[5,6] although this has been disputed.[7] The relevance of these findings to nursing mothers is not known. The prolactin level in a mother with established lactation may not affect her ability to breastfeed.

Alternate Drugs to Consider

Raltegravir

References

1.

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]

2.

García-Benayas T, Blanco F, Martin-Carbonero L, et al. Gynecomastia in HIV-infected patients receiving antiretroviral therapy. AIDS Res Hum Retroviruses. 2003;19:739–41. [PubMed: 14585204]

3.

Pantanowitz L, Evans D, Gross PD, et al. HIV-related gynecomastia. Breast J. 2003;9:131–2. [PubMed: 12603389]

4.

Evans DL, Pantanowitz L, Dezube BJ, et al. Breast enlargement in 13 men who were seropositive for human immunodeficiency virus. Clin Infect Dis. 2002;35:1113–9. [PubMed: 12384846]

5.

Hutchinson J, Murphy M, Harries R, et al. Galactorrhoea and hyperprolactinaemia associated with protease-inhibitors. Lancet. 2000;356:1003–4. [PubMed: 11041407]

6.

Orlando G, Brunetti L, Vacca M. Ritonavir and saquinavir directly stimulate anterior pituitary prolactin secretion, in vitro. Int J Immunopathol Pharmacol. 2002;15:65–8. [PubMed: 12593790]

7.

Montero A, Bottasso OA, Luraghi MR, et al. Galactorrhoea, hyperprolactinaemia, and protease inhibitors. Lancet. 2001;357:473–4. [PubMed: 11273087]

Substance Name

Bictegravir

CAS Registry Number

1611493-60-7

Drug Class

Breast Feeding

Lactation

Milk, Human

Antiviral Agents

Anti-HIV Agents

Anti-Retroviral Agents

HIV Integrase Inhibitors