Sunlenca® (lenacapavir)

Alternative Sites of Administration

This document is in response to your request for information regarding subcutaneous Sunlenca® (lenacapavir [LEN]) and alternative sites of subcutaneous (SUBQ) administration other than the abdomen.

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: www.gilead.com/-/media/files/pdfs/medicines/hiv/sunlenca/sunlenca_pi.

Product Labeling1

There is no information in the LEN US FDA-approved Prescribing Information on alternative sites of administration.

Dosage and Administration

Preparation and administration of SUBQ injection

LEN injection is only for SUBQ administration into the abdomen by a healthcare provider. Do NOT administer intradermally due to risk of serious injection site reactions. Refer to the prescribing information for additional information regarding the recommended injection steps.

Clinical Studies on the Administration of LEN in Alternative Sites

Phase 1 PK Study: Administration in Alternative Sites2

Study design and demographics

A phase 1, open-label, parallel-design, single-dose, multicohort study evaluated the PK and safety of LEN administered SUBQ in different sites.2,3 Healthy adult volunteers aged 18 to 55 years who had a BMI of 19 to 30 kg/m2 were enrolled into one of four cohorts (n=10 per cohort). Each cohort of healthy volunteers received a single 927 mg dose of LEN SUBQ administered as two 1.5 mL injections either bilaterally in the thigh, upper arm, or gluteal region or in two different abdominal quadrants, which is the approved administration site and served as a reference. PK samples from plasma were collected post dose at Hours 0, 2, 4, 6, 8, 12, 24, 36, 48, 72, 96, 120, 144, 168, 192, and 216, followed by weekly or biweekly assessments between Days 15 and 210 and monthly assessments through to Day 270.2 Safety evaluations included injection site examinations on Days 1 to 10 and at each study visit through Day 270 to evaluate the occurrence of ISRs.3 Baseline demographics were generally similar among cohorts (Table 1).2

Table 1. Baseline Demographics (Lat et al)2

PK results2

Exposures to LEN after SUBQ administration into the thigh, upper arm, and gluteal regions were generally similar or slightly higher than those observed after administration into the abdomen; observed PK differences were not considered clinically significant (Table 2). GM Cmax, AUC6 mo, and AUClast values were 8% to 15% lower after SUBQ administration into the thigh than those observed for the abdomen (reference comparator) cohort; these PK parameters were 5% to 33% higher in the upper-arm cohort and 18% to 26% higher in the gluteal-region cohort than in the abdomen cohort. The GM C6 mo in each cohort was greater than the IQ4 (target efficacy concentration) of 15.5 ng/mL.

Table 2. PK Parameters by Administration Site (Lat et al)2

Abbreviations: %CV=geometric % coefficient of variation; AUC∞=area under the concentration-time curve to infinity; Q=quartile; T1/2=half-life; Tmax=time to Cmax.

aThree healthy volunteers (abdomen, n=2; gluteal region, n=1) were lost to follow-up or withdrew prematurely.

bAUC∞ and T1/2, n=6; AUClast and AUC6 mo, n=9.

Safety results3

No serious AEs or AEs that resulted in study discontinuation occurred. Treatment-related AEs occurred in 38/40 participants (95%), and all non-ISR treatment-related AEs were Grade 1. Most participants (38/40; 95%) experienced ISRs, and the most common ISRs were pain (90%), induration (73%), erythema (70%), nodules (15%), and swelling (15%; Table 3). All ISRs were Grade ≤2 except for 1 event of erythema in the upper-arm cohort.

Table 3. Most Common ISRs by Administration Site (Saunders et al)3

References

1. SUNLENCA® (lenacapavir) tablets, for oral use. SUNLENCA® (lenacapavir) injection, for subcutaneous use. US Prescribing Information. Foster City, CA.
2. Lat A, Kim A, Zhang H, et al. Impact of Subcutaneous Administration Sites on the Clinical Pharmacokinetics of Lenacapavir , a Long-Acting HIV Capsid Inhibitor: Does Body Site Matter?. [Poster 1542]. Paper presented at: ID Week 2023; October 11-15, 2023; Boston, MA.
3. Saunders G, Mortensen E, Shen G, Kim A. Injection Site Reactions with Subcutaneous Lenacapavir Administration at Alternate Injection Sites [Poster THPEB103]. Paper presented at: 25th International AIDS Conference; July 22-26, 2024; Munich, Germany.

Abbreviations

AE=adverse event
AUC6 mo=area under the concentration-time curve at 6 months
AUClast=area under the concentration-time curve from dosing to last measurable concentration
C6 mo=concentration at 6 months
Cmax=maximum concentration
GM=geometric mean
ISR=injection site reaction
IQ4=inhibitory quotient-4
LEN=lenacapavir
PK=pharmacokinetic(s)
SUBQ=subcutaneous(ly)

Product Label

For the full indication, important safety information, and boxed warning(s), please refer to the Sunlenca US Prescribing Information available at:
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
 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.