Sunlenca® (lenacapavir)

Coadministration with Rifampin

This document is in response to your request for information regarding Sunlenca® (lenacapavir [LEN]) and coadministration with rifampin (RIF).

Some data may be outside of the US FDA-approved Prescribing Information. In providing this data, Gilead Sciences, Inc. is not making any representation as to its clinical relevance or to the use of any Gilead product(s). For information about the approved conditions of use of any Gilead drug product, please consult the FDA approved prescribing information.

The full indication, important safety information, and boxed warnings are available at: http://www.gilead.com/-/media/files/pdfs/medicines/hiv/sunlenca/sunlenca_pi

PK DDI Evaluation

Concomitant administration of LEN with RIF is contraindicated. Concomitant administration of LEN with RIF may decrease LEN concentrations, and may result in loss of therapeutic effect and development of resistance.1

LEN PK1,2

aCombined P‑gp, UGT1A1, and strong CYP3A inhibitors may significantly increase plasma concentrations of LEN. Concomitant administration of LEN with these inhibitors is not recommended.

bDrugs that are strong or moderate inducers of CYP3A may significantly decrease plasma concentrations of LEN, which may result in loss of therapeutic effect of LEN and development of resistance. Concomitant administration of LEN with strong CYP3A inducers during LEN treatment is contraindicated. Concomitant administration of LEN with moderate CYP3A inducers during LEN treatment is not recommended.

Relevant LEN Label Information1

Concomitant administration of LEN with RIF may decrease LEN concentrations, and may result in loss of therapeutic effect and development of resistance. Concomitant administration of LEN with RIF is contraindicated.

Table 1. Effect of RIF on LEN

Available Data

There are no Gilead studies evaluating the clinical outcomes of the coadministration of LEN with RIF.

A literature search was conducted in Ovid MEDLINE, BIOSIS Previews, and Embase databases for studies published between 1946 and December 23, 2024 using search terms that included Sunlenca, lenacapavir, rifampin, and related search terms. No relevant citations were found.

References

1. Enclosed, Gilead Sciences Inc. SUNLENCA® (lenacapavir) tablets, for oral use. SUNLENCA® (lenacapavir) injection, for subcutaneous use. U.S. Prescribing Information. Foster City, CA.
2. Lutz J. CLINICAL EVALUATION OF DRUG INTERACTIONS WITH ORAL LENACAPAVIR AND PROBE DRUGS [Presentation]. Paper presented at: Conference on Retroviruses and Opportunistic Infections (CROI); March 6-10, 2021; Virtual.

Abbreviations

AUC=area under the curve

BCRP=breast cancer resistance protein

Cmax=maximal concentration

DDI=drug-drug interaction

LEN=lenacapavir

MATE=multidrug and toxin extrusion protein

NA=not applicable
OATP=organic anion transporting polypeptide

OCT=organic cation transporter

P-gp=P-glycoprotein

PK=pharmacokinetic(s)
RIF=rifampin
UGT=uridine 5’-diphospho- glucuronosyltransferase
 

Product Label

For the full indication, important safety information, and boxed warning(s), please refer to the Sunlenca US Prescribing Information available at:
http://www.gilead.com/-/media/files/pdfs/medicines/hiv/sunlenca/sunlenca_pi.

Follow-Up

For any additional questions, please contact Gilead Medical Information at:

☎1‐866‐MEDI‐GSI (1‐866‐633‐4474) or   www.askgileadmedical.com

Adverse Event Reporting

Please report all adverse events to:

Gilead Global Patient Safety ☎ 1-800-445-3235, option 3 or
 https://www.gilead.com/utility/contact/report-an-adverse-event

FDA MedWatch Program by ☎ 1-800-FDA-1088 or MedWatch, FDA, 5600 Fishers Ln, Rockville, MD 20852 or   www.accessdata.fda.gov/scripts/medwatch

Data Privacy

The Medical Information service at Gilead Sciences may collect, store and use your personal information to provide a response to your medical request.  We may share your information with other Gilead Sciences colleagues to ensure that your request is addressed appropriately.  If you report an adverse event or concern about the quality of a Gilead or Kite product, we will need to use the information you have given us in order to meet our regulatory requirements in relation to the safety of our medicines.

It may be necessary for us to share your information with Gilead’s affiliates, business partners, service providers and regulatory authorities located in countries besides your own.  Gilead Sciences has implemented measures to protect the personal information you provide.  Please see the Gilead Privacy Statement (www.gilead.com/privacy-statements) for more information about how Gilead handles your personal information and your rights.  If you have any further questions about the use of your personal information, please contact privacy@gilead.com.

SUNLENCA, GILEAD, and the GILEAD logo are registered trademarks of Gilead Sciences, Inc., or its related companies.
© 2024 Gilead Sciences, Inc.