Sunlenca LENACAPAVIR SODIUM Kit
🆔 Identity & classification
Where does this data come from?
🏷️ RxNorm drug class
This medicine belongs to the Human Immunodeficiency Virus 1 Capsid Inhibitor class.
Where does this data come from?
🏭 Manufacturer & labeler
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🩺 Clinical
Lenacapavir injection is used to treat human immunodeficiency virus (HIV). Lenacapavir is also used along with practicing safer sex (e.g., condom use) to reduce the risk of HIV infection. Lenacapavir is in a class of medications called HIV capsid inhibitors. It works by decreasing the amount of HIV in the blood. Although lenacapavir does not cure HIV, it may decrease your chance of developing acquired immunodeficiency syndrome (AIDS) and HIV-related illnesses. Taking these medications along with practicing safer sex and making other life-style changes may decrease the risk of giving the HIV v...
Read the full MedlinePlus article ↗- Great question. The tablets are a short-term loading dose — they're taken on specific days right at the start of your therapy to quickly build up enough lenacapavir in your system...
- Why do I need to take tablets if lenacapavir is supposed to be a shot?
- Yes — you can take it with or without food. There's no requirement to fast or eat a specific meal beforehand. Just take it as your prescriber directed.
- Can I eat before taking my lenacapavir tablet?
Patient education
Supplement & herbal interactions
Where does this data come from?
Ask a licensed pharmacist directly — free, answered by our team.
💊 What it looks like
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🧪 Inactive Ingredients / Excipients
Inactive ingredients, also called excipients, are components of the drug product other than the active ingredient. They may include fillers, dyes, coatings, preservatives, flavors, or other formulation ingredients.
Where does this data come from?
IACT rows and label-wide narrative are kept separate; availability and product-level specificity depend on the submitted label.Inactive ingredient FAQ
Are inactive ingredients the same for every manufacturer?
Why might an inactive ingredient be missing?
Can inactive ingredients matter?
💲 Pricing
A drug doesn't have one price. Each row is a different public payment system, and none is what you'd pay at the counter — that depends on your insurance. The ⓘ on each row explains what it measures.
| Price system | Per each | Per package |
|---|---|---|
| Retail pharmacies payNADAC · weekly | Not in the retail survey — common for institutional, discontinued, or low-volume packs. | |
| Medicaid paysCMS SDUD · 12 mo | $8,721.39 | — |
| Medicare drug plans payPart D · Q2 2026 | $812.00 | — |
| Medicare Part B allowsASP · J1961 | $22.936 / J1961 unit | — |
Where does this data come from?
🧾 Billing & reimbursement
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🔁 Therapeutic equivalents
| Product | Labeler | Pack | NADAC/unit | TE | Status | Price vs. this |
|---|---|---|---|---|---|---|
| Sunlenca 61958-3002-01 | Gilead | 1 kit | — | — | FDA listed | — |
| Sunlencathis 61958-3005-01 | Gilead | 1 kit | — | — | FDA listed | — |
| Yeztugo 61958-3402-01 | Gilead | 1 kit | — | — | FDA listed | — |
Where does this data come from?
⏳ Availability & generic status
We did not find an FDA-approved generic match for this exact strength, form and route. Patent/protection dates below may affect future generic timing.
Why the date isn’t exact: Generic timing can change because patents may be challenged, settled, licensed, added, removed, or worked around with a narrower label — and FDA approval does not always mean a pharmacy can get the generic today.
🛈 What do these terms mean?
- Patent
- Legal protection listed in the Orange Book that may delay generic approval or launch. Issued by the U.S. Patent & Trademark Office.
- Substance patent
- Covers the active drug molecule itself — the hardest to design around. A generic generally can’t launch until it expires.
- Formulation (product) patent
- Covers a specific formulation or dosage form. A generic can sometimes work around it with a different formulation.
- Method-of-use patent
- A patent covering one specific approved use of the drug — not necessarily the whole molecule. A generic can sometimes launch with a “skinny label” that carves out the protected use and keeps the others.
- Skinny label
- A generic label that omits a still-patented use when the FDA allows it — letting a generic reach the market for the unprotected uses.
- Exclusivity
- FDA-granted marketing protection, separate from patents — e.g. 5-yr new chemical entity, 7-yr orphan drug, or a +6-month pediatric extension.
- Paragraph IV
- A generic applicant’s formal challenge to a listed patent. It can potentially lead to earlier generic entry, but often involves litigation or a settlement.
- RLD / RS
- Reference Listed Drug — the brand product the FDA uses as the reference for generic applications. Reference Standard — the product the FDA expects generics to compare against in bioequivalence testing.
- TE / AB rating
- FDA therapeutic-equivalence rating. An AB rating generally means the FDA considers a generic therapeutically equivalent to — and substitutable for — the brand.
- LOE (loss of exclusivity)
- The latest patent or exclusivity currently listed — the loss-of-exclusivity / latest-listed-protection date shown on this page. Paragraph-IV challenges and settlements can move the real date earlier; FDA approval and a manufacturer’s decision to market can move it later.
Built from the FDA Orange Book. The bars above are scaled to each protection’s expiry; the red LOE marker is the last one to lapse.
| Patent | Type | Use code | Expires |
|---|---|---|---|
| US 11944611 ↗ | Method of use | U-3507 | Aug 28, 2041 |
| US 10654827 ↗ | Method of use | U-3507 | Aug 17, 2037 |
| US 9951043 ↗ | Drug substance | U-3507 | Feb 28, 2034 |
| US 12594267 ↗ | Drug product | — | Jul 15, 2039 |
| US 10071985 ↗ | Drug substance | — | Aug 17, 2037 |
| US 11267799 ↗ | Drug substance | — | Aug 16, 2038 |
| Code | What it grants | Expires |
|---|---|---|
| NCE | New Chemical Entity (5-year) | Dec 22, 2027 |
Is there a generic version of SUNLENCA 463.5 MG/1.5 ML VIAL?
The FDA approved a generic — why can’t I get it at my pharmacy yet?
Why do different websites show different generic release dates?
What does “FDA listed” mean?
What does a patent or protection date mean here?
What does “current Orange Book estimate” mean?
Can a generic come out before the last patent expires?
Can a generic come out after the listed dates?
What is the difference between patents and exclusivity?
Why are there multiple patent dates?
Where does this data come from?
🗺️ Medicaid utilization & spend
📊 Medicare Part D spend CMS · PART D · 2026 (Q1)
🔬 Reported adverse events (FAERS)
Top reported reactions
Age at onset
Reporter sex
Serious outcomes
Where does this data come from?
📦 Packaging — all sizes for this product
| Package NDC | Description | Marketing start | Status |
|---|---|---|---|
| 61958-3005-01 You're viewing this | 1 KIT in 1 CARTON (61958-3005-1) * 1.5 mL in 1 VIAL (61958-3004-1) | 2025-03-18 | Active |
🧭 About this NDC listing & data coverage
Kit / multi-component package
This NDC identifies a kit — a package containing more than one component. Structured data (pricing, ingredients, equivalents) is often reported per component rather than for the kit NDC itself, which can make this page look thinner than the components' own pages.
What data is (and isn’t) available for this NDC — tap to expand
| NDC identity (package / product / labeler codes) | ✓ Available |
| Labeler | ✓ Available |
| Product & package description | ✓ Available |
| Marketing category & status | ✓ Available |
| Active ingredient / dosage form / route | ✓ Available |
| FDA label (SPL via DailyMed) | ✓ Available |
| Package photos | ✓ Available |
| Inactive ingredients (structured) | — Not published for this NDC The labeler did not submit a structured excipient list, or no SPL is available. |
| NADAC pharmacy acquisition price (CMS) | — Not published for this NDC CMS publishes NADAC only for NDCs reported in its retail-pharmacy survey. |
| Orange Book / therapeutic-equivalence data | ✓ Available |
| HCPCS J-code billing crosswalk | ✓ Available |
| Medicaid utilization (CMS SDUD) | ✓ Available |
Questions about this listing
Why is there no price listed?
Is the NDC printed on the package the same as the 11-digit billing NDC?
What do the three segments of this NDC mean?
Is this package still being marketed?
Who lists this product with the FDA?
Do I need a prescription for this product?
Does this product have a billing J-code?
Where does this data come from?
📄 Full prescribing information FDA SPL
🎯 Indications and Usage ▾
1 INDICATIONS AND USAGE SUNLENCA, a human immunodeficiency virus type 1 (HIV-1) capsid inhibitor, is indicated: in combination with other antiretroviral(s), for the treatment of HIV-1 infection in heavily treatment-experienced adults with multidrug resistant HIV-1 whose current antiretroviral regimen is failing due to resistance, intolerance, or safety considerations. ( 1.1 ) for oral loading as a component of the initiation regimen for BIXLENVO (bictegravir [BIC]/lenacapavir [LEN]), a complete regimen for the treatment of HIV-1 infection, in adults to replace the current antiretroviral regimen in those who are virologically suppressed (HIV-1 RNA less than 50 copies per mL) on a stable antiretroviral regimen with no known or suspected resistance to the individual components of BIXLENVO.
( 1.2 )
1.1Treatment of HIV-1 in Heavily Treatment-Experienced Adults SUNLENCA, in combination with other antiretroviral(s), is indicated for the treatment of human immunodeficiency virus type 1 (HIV-1) infection in heavily treatment-experienced adults with multidrug resistant HIV-1 whose current antiretroviral regimen is failing due to resistance, intolerance, or safety considerations.
1.2Oral Loading for Initiation of BIXLENVO SUNLENCA tablets are indicated for oral loading as a component of the initiation regimen for BIXLENVO (bictegravir [BIC]/lenacapavir [LEN]), a complete regimen for treatment of HIV-1 infection, in adults to replace the current antiretroviral regimen in those who are virologically suppressed (HIV-1 RNA less than 50 copies per mL) on a stable antiretroviral regimen with no known or suspected resistance to the individual components of BIXLENVO [see Dosage and Administration (2.3) ] .
⏱️ Dosage and Administration ▾
2 DOSAGE AND ADMINISTRATION Recommended dosage in heavily treatment-experienced adults: Initiation with one of two options followed by once every 6 months maintenance injection dosing. Tablets may be taken without regard to food. ( 2.2 ) Initiation Option 1 Day 1 927 mg by subcutaneous injection (2 × 1.5 mL injections) 600 mg orally (2 × 300 mg tablets) Day 2 600 mg orally (2 × 300 mg tablets) Initiation Option 2 Day 1 600 mg orally (2 × 300 mg tablets) Day 2 600 mg orally (2 × 300 mg tablets) Day 8 300 mg orally (1 × 300 mg tablet) Day 15 927 mg by subcutaneous injection (2 × 1.5 mL injections) Maintenance 927 mg by subcutaneous injection (2 × 1.5 mL injections) every 6 months (26 weeks) from the date of the last injection +/-2 weeks.
Recommended dosage for oral loading for initiation of BIXLENVO: Refer to Table 3 of the full prescribing information for dosing schedule. ( 2.3 ) Planned missed injections: If scheduled injection is to be missed by more than 2 weeks, SUNLENCA tablets may be used for oral bridging for up to 6 months until injections resume. Recommended dosage is 300 mg orally once every 7 days.
( 2.4 ) Unplanned missed injections: If more than 28 weeks have elapsed since last injection and tablets have not been taken for oral bridging, restart initiation from Day 1 (using Option 1 or Option 2) if clinically appropriate. ( 2.4 ) SUNLENCA injection is for subcutaneous administration only. Two 1.5 mL injections are required for complete dose.
( 2.5 )
2.1Adherence to Treatment Regimen in Heavily Treatment-Experienced Adults Prior to starting SUNLENCA for the treatment of HIV-1 in heavily treatment-experienced adults, healthcare providers should carefully select patients who agree to the required every 6 month injection dosing schedule and counsel patients about the importance of adherence to scheduled SUNLENCA dosing visits and concomitant oral antiretroviral therapy to help maintain viral suppression and reduce the risk of viral rebound and potential development of resistance with missed doses [see Warnings and Precautions (5.2) , Microbiology (12.4) ] .
2.2Recommended Dosage for Treatment of HIV-1 in Heavily Treatment-Experienced Adults SUNLENCA can be initiated using one of the two recommended dosage regimens in Table 1 and Table 2 below. Maintenance dosing is administered by subcutaneous injection every 6 months regardless of the initiation regimen. Healthcare providers should determine the appropriate initiation regimen for the patient.
SUNLENCA oral tablets may be taken with or without food [see Clinical Pharmacology (12.3) ] . Table 1 Recommended Treatment Regimen for SUNLENCA Initiation and Maintenance for Treatment of HIV-1 in Heavily Treatment-Experienced Adults, Option 1 Treatment Time Dosage of SUNLENCA: Initiation Day 1 927 mg by subcutaneous injection (2 × 1.5 mL injections) and 600 mg orally (2 × 300 mg tablets) Day 2 600 mg orally (2 × 300 mg tablets) Dosage of SUNLENCA: Maintenance Every 6 months (26 weeks) From the date of the last injection. +/-2 weeks 927 mg by subcutaneous injection (2 × 1.5 mL injections) Table 2 Recommended Treatment Regimen for SUNLENCA Initiation and Maintenance for Treatment of HIV-1 in Heavily Treatment-Experienced Adults, Option 2 Treatment Time Dosage of SUNLENCA: Initiation Day 1 600 mg orally (2 × 300 mg tablets) Day 2 600 mg orally (2 × 300 mg tablets) Day 8 300 mg orally (1 × 300 mg tablet) Day 15 927 mg by subcutaneous injection (2 × 1.5 mL injections) Dosage of SUNLENCA: Maintenance Every 6 months (26 weeks) From the date of the last injection. +/-2 weeks 927 mg by subcutaneous injection (2 × 1.5 mL injections)
2.3Recommended Dosage for Oral Loading for Initiation of BIXLENVO SUNLENCA tablets are used as a component of the initiation regimen for BIXLENVO. See BIXLENVO prescribing information. The BIXLENVO dosing schedule in adults requires a two-day initiation regimen of BIXLENVO tablets plus SUNLENCA tablets taken orally, followed by a maintenance regimen of one…
💊 Dosage Forms and Strengths ▾
3 DOSAGE FORMS AND STRENGTHS Tablets: 300 mg Injection: 463.5 mg/1.5 mL (309 mg/mL) in single-dose vials. ( 3 ) SUNLENCA tablets: Each tablet contains 300 mg of lenacapavir. The tablets are beige, capsule-shaped, film-coated, and debossed with 'GSI' on one side of the tablet and '62L' on the other side of the tablet.
SUNLENCA injection: Each single-dose vial contains 463.5 mg/1.5 mL (309 mg/mL) of lenacapavir. The lenacapavir injectable solution is sterile, preservative-free, clear, and yellow with no visible particles.
⛔ Contraindications ▾
4 CONTRAINDICATIONS Concomitant administration of SUNLENCA with strong CYP3A inducers is contraindicated due to decreased lenacapavir plasma concentrations, which may result in the loss of therapeutic effect and development of resistance to SUNLENCA [see Drug Interactions (7.1) ] . Concomitant administration of SUNLENCA is contraindicated with strong CYP3A inducers. ( 4 )
⚠️ Warnings and Cautions ▾
5 WARNINGS AND PRECAUTIONS Immune reconstitution syndrome: May necessitate further evaluation and treatment. ( 5.1 ) Residual concentrations of lenacapavir may remain in systemic circulation for up to 12 months or longer. Counsel patients regarding the dosing schedule; non-adherence could lead to loss of virologic response and development of resistance.
( 5.2 ) May increase exposure and risk of adverse reactions to drugs primarily metabolized by CYP3A initiated within 9 months after the last subcutaneous dose of SUNLENCA. ( 5.2 ) If discontinued, initiate an alternative, fully suppressive antiretroviral regimen where possible no later than 28 weeks after the final injection of SUNLENCA. If virologic failure occurs, switch to an alternative regimen if possible.
( 5.2 ) Injection site reactions may occur, and nodules and indurations may be persistent. Improper administration (intradermal injection) has been associated with serious injection site reactions. ( 5.3 )
5.1Immune Reconstitution Syndrome Immune reconstitution syndrome has been reported in patients treated with combination antiretroviral therapy. During the initial phase of combination antiretroviral treatment, patients whose immune system responds may develop an inflammatory response to indolent or residual opportunistic infections [such as Mycobacterium avium infection, cytomegalovirus, Pneumocystis jirovecii pneumonia (PCP), or tuberculosis], which may necessitate further evaluation and treatment. Autoimmune disorders (such as Graves' disease, polymyositis, Guillain-Barré syndrome, and autoimmune hepatitis) have also been reported to occur in the setting of immune reconstitution; however, the time to onset is more variable, and can occur many months after initiation of treatment.
5.2Long-Acting Properties and Potential Associated Risks with SUNLENCA Residual concentrations of lenacapavir may remain in the systemic circulation of patients for prolonged periods (up to 12 months or longer after the last subcutaneous dose). It is important to counsel patients that maintenance dosing by injection is required every 6 months, because missed doses or non-adherence to injections could lead to loss of virologic response and development of resistance [see Dosage and Administration (2.1) ] . Lenacapavir, a moderate CYP3A inhibitor, may increase the exposure to, and therefore potential risk of adverse reactions from, drugs primarily metabolized by CYP3A initiated within 9 months after the last subcutaneous dose of SUNLENCA [see Drug Interactions and Clinical Pharmacology (7.2 , 12.3) ] .
If SUNLENCA is discontinued, to minimize the potential risk of developing viral resistance, it is essential to initiate an alternative, fully suppressive antiretroviral regimen where possible no later than 28 weeks after the final injection of SUNLENCA. If virologic failure occurs during treatment, switch the patient to an alternative regimen if possible [see Dosage and Administration (2.1) ].
5.3Injection Site Reactions Administration of SUNLENCA may result in local injection site reactions (ISRs). If clinically significant ISRs occur, evaluate and institute appropriate therapy and follow-up. Manifestations of ISRs may include swelling, pain, erythema, nodule, induration, pruritus, extravasation or mass.
Nodules and indurations at the injection site may take longer to resolve than other ISRs. In clinical studies, after a median follow-up of 553 days, 30% of nodules and 13% of indurations (in 10% and 1% of participants, respectively) associated with the first injections of SUNLENCA had not fully resolved. Measurements and qualitative assessments of ISRs were not routinely reported.
Where described, the majority of the injection site nodules and indurations were palpable but not visible, and had a maximum size of approximately 1 to 4 cm [see Adverse Reactions (6.1) ] . The mechanism driving the persistence of injection site nodules and indurations in some patients is not fully understood, but b…
🤒 Adverse Reactions ▾
6 ADVERSE REACTIONS The following adverse reactions are discussed in other sections of the labeling: Immune Reconstitution Syndrome [see Warnings and Precautions (5.1) ] Injection Site Reactions [see Warnings and Precautions (5.3) ]. Most common adverse reactions (incidence greater than or equal to 3%, all grades) are nausea and injection site reactions. ( 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact Gilead Sciences, Inc. at 1-800-GILEAD-5 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch.
6.1Clinical Trials Experience Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice. Treatment of HIV-1 in Heavily Treatment-Experienced Adults The primary safety assessment of SUNLENCA was based on data from heavily treatment-experienced adult participants with HIV who received SUNLENCA in a Phase 2/3 trial (CAPELLA; N=72) through Week 52 (median duration on study of 71 weeks) [see Clinical Studies (14.1) ] , as well as supportive data in treatment-naïve adult participants with HIV who received SUNLENCA in a Phase 2 trial (CALIBRATE; N=157) through Week 54 (median duration of exposure of 66 weeks).
The most common adverse reactions (all Grades) reported in at least 3% of participants in CAPELLA were nausea and injection site reactions. The proportion of participants in CAPELLA who discontinued treatment with SUNLENCA due to adverse events, regardless of severity, was 1% (Grade 1 injection site nodule in 1 participant). Table 6 displays the frequency of adverse reactions (all Grades) greater than or equal to 3% in the SUNLENCA group.
Table 6 Adverse Reactions (All Grades) Reported in ≥ 3% Frequencies of adverse reactions are based on all adverse events attributed to trial drug by the investigator, based on all participants (cohorts 1 and 2) in CAPELLA. of Heavily Treatment Experienced Adults with HIV-1 Receiving SUNLENCA in CAPELLA (Week 52 Analysis) Adverse Reactions SUNLENCA + Background Regimen (N=72) Injection Site Reactions 65% Nausea 4% The majority (96%) of all adverse reactions associated with SUNLENCA were mild or moderate in severity. Injection-Associated Adverse Reactions Local Injection Site Reactions (ISRs) : The most frequent adverse reactions were ISRs.
Of the 72 participants in CAPELLA, 65% had experienced an ISR attributed to study drug through at least the Week 52 visit. Most participants had mild (Grade 1, 44%) or moderate (Grade 2, 17%) ISRs. Four percent of participants experienced a severe (Grade 3) ISR (erythema, pain, swelling) that resolved within 15 days.
The ISRs reported in more than 1% of participants were swelling (36%), pain (31%), erythema (31%), nodule (25%), induration (15%), pruritus (6%), extravasation (3%) and mass (3%). ISRs reported in 1% of participants included discomfort, hematoma, edema, and ulcer. Nodules and indurations at the injection site took longer to resolve than other ISRs.
The median time to resolution of all ISRs, excluding nodules and indurations, was 5 days (range: 1 to 183). The median time to resolution of nodules and indurations associated with the first injections of SUNLENCA was 148 (range: 41 to 727) and 70 (range: 3 to 252) days, respectively. After a median follow up of 553 days, 30% of nodules and 13% of indurations (in 10% and 1% of participants, respectively) associated with the first injections of SUNLENCA had not fully resolved.
Qualitative descriptions of injection site nodules and indurations were not routinely reported, but, where reported, the majority of injection site nodules and indurations were palpable but not visible. Measurements of injection site nodules and indurations were not routinely performed or standardized, but where measurements were reported, the maximum size for the majority of injection site nodules and indurations was approximately 1 to…
🔄 Drug Interactions ▾
7 DRUG INTERACTIONS Consult the Full Prescribing Information prior to and during treatment for important drug interactions. ( 4 , 7 , 12.3 )
7.1Effect of Other Drugs on SUNLENCA Lenacapavir is a substrate of P-gp, UGT1A1, and CYP3A. Strong or Moderate CYP3A Inducers Drugs that are strong or moderate inducers of CYP3A may significantly decrease plasma concentrations of lenacapavir [see Clinical Pharmacology (12.3) ] , which may result in loss of therapeutic effect of SUNLENCA and development of resistance. Concomitant administration of SUNLENCA with strong CYP3A inducers during SUNLENCA treatment is contraindicated [see Contraindications (4) ] .
Concomitant administration of SUNLENCA with moderate CYP3A inducers during SUNLENCA treatment is not recommended. Combined P-gp, UGT1A1, and Strong CYP3A Inhibitors Combined P-gp, UGT1A1, and strong CYP3A inhibitors may significantly increase plasma concentrations of SUNLENCA. Concomitant administration of SUNLENCA with these inhibitors is not recommended.
7.2Effect of SUNLENCA on Other Drugs Lenacapavir is a moderate inhibitor of CYP3A. Due to the long half-life of lenacapavir following subcutaneous administration, SUNLENCA may increase the exposure of drugs primarily metabolized by CYP3A [see Clinical Pharmacology (12.3) ] initiated within 9 months after the last subcutaneous dose of SUNLENCA, which may increase the potential risk of adverse reactions. See the prescribing information of the sensitive CYP3A substrate for dosing recommendations with moderate inhibitors of CYP3A.
7.3Established and Other Potentially Significant Drug Interactions Table 8 provides a listing of clinically significant drug interactions with recommended prevention or management strategies, but is not all inclusive. The drug interactions described are based on studies conducted with SUNLENCA or are drug interactions that may occur with SUNLENCA [see Contraindications (4) and Clinical Pharmacology (12.3) ] . Table 8 Drug Interactions with SUNLENCA Concomitant Drug Class: Drug Name Effect on Concentration ↑ = Increase, ↓ = Decrease.
Clinical Comment Antiarrhythmics: digoxin ↑ digoxin Use with caution and monitor digoxin therapeutic concentration. Anticoagulants: Direct Oral Anticoagulants (DOACs) rivaroxaban dabigatran edoxaban ↑ DOAC Refer to the DOAC prescribing information for concomitant administration with moderate CYP3A inhibitors and/or P-gp inhibitors. Anticonvulsants: carbamazepine oxcarbazepine phenobarbital phenytoin ↓ lenacapavir Concomitant administration of carbamazepine, oxcarbazepine, phenobarbital, or phenytoin may result in loss of therapeutic effect and development of resistance.
Concomitant administration of SUNLENCA with carbamazepine or phenytoin is contraindicated. Concomitant administration of SUNLENCA with oxcarbazepine or phenobarbital is not recommended. Consider use of alternative anticonvulsants.
Antiretroviral Agents: atazanavir/cobicistat Drug-drug interaction study was conducted. atazanavir/ritonavir ↑ lenacapavir (atazanavir/cobicistat, atazanavir/ritonavir) Concomitant administration of efavirenz, nevirapine, or tipranavir/ritonavir may result in loss of therapeutic effect and development of resistance. efavirenz nevirapine tipranavir/ritonavir ↓ lenacapavir (efavirenz, nevirapine, tipranavir/ritonavir) Concomitant administration with atazanavir/cobicistat, atazanavir/ritonavir, efavirenz, nevirapine, or tipranavir/ritonavir is not recommended.
Antimycobacterials: rifabutin rifampin rifapentine ↓ lenacapavir Concomitant administration of rifabutin, rifampin and rifapentine may result in loss of therapeutic effect and development of resistance. Concomitant administration of SUNLENCA with rifampin is contraindicated [see Contraindications (4) ] . Concomitant administration of SUNLENCA with rifabutin or rifapentine is not recommended.
Corticosteroids (systemic): cortisone/hydrocortisone dexamethasone ↑ corticosteroids (systemic) Concomitant administration with systemic corticost…
👥 Use in Specific Populations ▾
8 USE IN SPECIFIC POPULATIONS
8.1Pregnancy Pregnancy Exposure Registry There is a pregnancy exposure registry that monitors pregnancy outcomes in individuals exposed to SUNLENCA during pregnancy. Healthcare providers are encouraged to register patients by calling the Antiretroviral Pregnancy Registry (APR) at 1-800-258-4263. Risk Summary Available data from a randomized, controlled trial with lenacapavir use during pregnancy in individuals without HIV-1 have not identified a drug-associated risk for miscarriage, or adverse maternal or fetal outcomes when compared to an active control (see Data ) .
The rate of major birth defects in lenacapavir-exposed pregnancies did not exceed the background prevalence rates. The risk estimates are imprecise due to small numbers of exposed pregnancies (see Data ) . In animal reproduction studies, no adverse developmental effects were observed when lenacapavir was administered to rats and rabbits at exposures (AUC) ≥16 times the exposure in humans at the recommended human dose (RHD) of SUNLENCA (see Data ) .
The background risk of major birth defects and miscarriage for the indicated population is unknown. The background rate of major birth defects in a U.S. reference population of the Metropolitan Atlanta Congenital Defects Program (MACDP) is 2.7%. The rate of miscarriage is not reported in the APR.
The estimated background rate of miscarriage in clinically recognized pregnancies in the U.S. general population is 15 to 20%. Data Human Data In a randomized, controlled trial of individuals without HIV-1 in Uganda and South Africa, there were 208 pregnancies exposed to lenacapavir with known outcomes and 132 deliveries (both live and non-live). In the active control arm of this trial, there were 109 pregnancies with known outcomes and 61 deliveries (both live and non-live).
The adverse pregnancy outcomes of spontaneous abortion, stillbirth, preterm birth, and small for gestational age were similar across both treatment groups. There were two major birth defects in the lenacapavir arm. Both were ventricular septal defects.
This resulted in a rate of major birth defects that fell within the background prevalence rate for major birth defects. Concentrations of lenacapavir during each trimester of pregnancy and postpartum were comparable to those in non-pregnant participants. Animal Data Lenacapavir was administered intravenously to pregnant rabbits (up to 20 mg/kg/day on gestation days (GD) 7 to 19), orally to rats (up to 300 mg/kg/day on GD 6 to 17), and subcutaneously to rats (up to 300 mg/kg on GD 6).
No significant toxicological effects on embryo-fetal (rats and rabbits) or pre/postnatal (rats) development were observed at exposures (AUC) approximately 16 times (rats) and 39 times (rabbits) the exposure in humans at the RHD of SUNLENCA.
8.2Lactation Risk Summary Lenacapavir is present in human milk. Lenacapavir was detected at very low levels in infants who were breastfed by individuals who became pregnant while receiving lenacapavir (see Data ) . No adverse effects of lenacapavir in breastfed infants have been observed.
It is not known if lenacapavir affects milk production. Potential risks of breastfeeding include: (1) HIV-1 transmission (in infants without HIV-1), (2) developing viral resistance (in infants with HIV-1), and (3) adverse reactions in a breastfed infant similar to those seen in adults. Data Human data The median lenacapavir concentration in human breast milk to maternal plasma ratio in participants (n=8) who received lenacapavir was 0.63 (range: 0.29 to 1.90).
The median infant-to-mother plasma ratio for lenacapavir in infants (n=10) who were breastfed by individuals receiving lenacapavir from 0 to less than 13 weeks after delivery was 0.06 (range: 0.01 to 0.20).
8.4Pediatric Use The safety and effectiveness of SUNLENCA have not been established in pediatric patients.
8.5Geriatric Use Clinical studies of SUNLENCA did not include sufficient numbers of participants aged 65 an…
🤰 Pregnancy ▾
8.1Pregnancy Pregnancy Exposure Registry There is a pregnancy exposure registry that monitors pregnancy outcomes in individuals exposed to SUNLENCA during pregnancy. Healthcare providers are encouraged to register patients by calling the Antiretroviral Pregnancy Registry (APR) at 1-800-258-4263. Risk Summary Available data from a randomized, controlled trial with lenacapavir use during pregnancy in individuals without HIV-1 have not identified a drug-associated risk for miscarriage, or adverse maternal or fetal outcomes when compared to an active control (see Data ) .
The rate of major birth defects in lenacapavir-exposed pregnancies did not exceed the background prevalence rates. The risk estimates are imprecise due to small numbers of exposed pregnancies (see Data ) . In animal reproduction studies, no adverse developmental effects were observed when lenacapavir was administered to rats and rabbits at exposures (AUC) ≥16 times the exposure in humans at the recommended human dose (RHD) of SUNLENCA (see Data ) .
The background risk of major birth defects and miscarriage for the indicated population is unknown. The background rate of major birth defects in a U.S. reference population of the Metropolitan Atlanta Congenital Defects Program (MACDP) is 2.7%. The rate of miscarriage is not reported in the APR.
The estimated background rate of miscarriage in clinically recognized pregnancies in the U.S. general population is 15 to 20%. Data Human Data In a randomized, controlled trial of individuals without HIV-1 in Uganda and South Africa, there were 208 pregnancies exposed to lenacapavir with known outcomes and 132 deliveries (both live and non-live). In the active control arm of this trial, there were 109 pregnancies with known outcomes and 61 deliveries (both live and non-live).
The adverse pregnancy outcomes of spontaneous abortion, stillbirth, preterm birth, and small for gestational age were similar across both treatment groups. There were two major birth defects in the lenacapavir arm. Both were ventricular septal defects.
This resulted in a rate of major birth defects that fell within the background prevalence rate for major birth defects. Concentrations of lenacapavir during each trimester of pregnancy and postpartum were comparable to those in non-pregnant participants. Animal Data Lenacapavir was administered intravenously to pregnant rabbits (up to 20 mg/kg/day on gestation days (GD) 7 to 19), orally to rats (up to 300 mg/kg/day on GD 6 to 17), and subcutaneously to rats (up to 300 mg/kg on GD 6).
No significant toxicological effects on embryo-fetal (rats and rabbits) or pre/postnatal (rats) development were observed at exposures (AUC) approximately 16 times (rats) and 39 times (rabbits) the exposure in humans at the RHD of SUNLENCA.
🧒 Pediatric Use ▾
8.4Pediatric Use The safety and effectiveness of SUNLENCA have not been established in pediatric patients.
🧓 Geriatric Use ▾
8.5Geriatric Use Clinical studies of SUNLENCA did not include sufficient numbers of participants aged 65 and over to determine whether they respond differently from younger patients.
🆘 Overdosage ▾
10 OVERDOSAGE No data are available on overdose of SUNLENCA in patients. If overdose occurs, monitor the patient for evidence of toxicity. Treatment of overdose with SUNLENCA consists of general supportive measures including monitoring of vital signs as well as observation of the clinical status of the patient. As lenacapavir is highly bound to plasma proteins, it is unlikely to be significantly removed by dialysis.
🧬 Clinical Pharmacology ▾
12 CLINICAL PHARMACOLOGY
12.1Mechanism of Action SUNLENCA is an HIV-1 antiretroviral agent [see Microbiology (12.4) ] .
12.2Pharmacodynamics Exposure-Response In CAPELLA, oral loading doses (600 mg on Day 1 and Day 2, 300 mg on Day 8) followed by subcutaneous doses (927 mg every 6 months starting on Day 15) of SUNLENCA in heavily treatment-experienced participants with multiclass resistant HIV-1, efficacy outcomes (change in plasma HIV-1 RNA from Day 1 to Day 14, and percentage of participants with HIV-1 RNA less than 50 copies/mL at Week 26) were similar across the range of observed lenacapavir exposures. Cardiac Electrophysiology At supratherapeutic exposures of lenacapavir (9-fold higher than the therapeutic exposures of SUNLENCA), SUNLENCA does not prolong the QTcF interval to any clinically relevant extent.
12.3Pharmacokinetics The pharmacokinetic (PK) properties of lenacapavir are provided in Table 9 . The PK parameter estimates of SUNLENCA after oral and subcutaneous administration in heavily-treatment experienced participants with HIV-1 are provided in Table 10 . The estimated lenacapavir exposures are comparable between the two recommended dosing regimens.
Table 9 Pharmacokinetic Properties of Lenacapavir Oral Subcutaneous Absorption % Absolute bioavailability 6 to 10 100 Values reflect absolute bioavailability following subcutaneous administration of the 927 mg dose. T max Values reflect administration of lenacapavir with or without food. 4 hours 77 to 84 days Due to slow release from the site of subcutaneous administration, the absorption profile of subcutaneously administered lenacapavir is complex.
Effect of Food Effect of low-fat meal (relative to fasting) Values refer to geometric mean ratio [low-fat meal/fasting] in PK parameters and (90% confidence interval). Low fat meal is approximately 400 kcal, 25% fat. AUC inf ratio 98.6 (58.2,167.2) - C max ratio 115.8 (55.4, 242.1) - Effect of high-fat meal (relative to fasting) Values refer to geometric mean ratio [high-fat meal/fasting] in PK parameters and (90% confidence interval).
High fat meal is approximately 1000 kcal, 50% fat. AUC inf ratio 115.2 (72.0, 184.5) - C max ratio 145.2 (77.9, 270.5) - Distribution Apparent volume of distribution (Vd/F, L) 19240 9500 to 11700 % bound to human plasma proteins >98.5 Blood-to-plasma ratio 0.5 to
0.7Values reflect the blood-to-plasma ratio of lenacapavir following a single dose intravenous administration of [ 14 C] lenacapavir through 336 hours postdose. Elimination t 1/2 10 to 12 days 8 to 12 weeks Clearance (mean apparent clearance, L/h) 55 4.2 % of dose of unchanged drug in plasma Dosing in mass balance studies: single dose intravenous administration of [ 14 C] lenacapavir to participants without HIV-1. 69 Metabolism Metabolic pathway(s) CYP3A (minor) UGT1A1 (minor) Excretion Major routes of elimination Excretion of unchanged drug into feces Metabolized via oxidation, N-dealkylation, hydrogenation, amide hydrolysis, glucuronidation, hexose conjugation, pentose conjugation, and glutathione conjugation; primarily via CYP3A and UGT1A1 and no single circulating metabolite accounted for >10% of plasma drug-related exposure. % of dose excreted in urine <1 % of dose excreted in feces (% unchanged) 76 (33) Table 10 Lenacapavir Exposures Following Oral and Subcutaneous Administration of SUNLENCA in Heavily Treatment Experienced Participants with HIV-1 Parameter Mean (%CV) Recommended Dosing Regimen, Option 1 Predicted exposures utilizing population PK analysis.
Recommended Dosing Regimen, Option 2 Day 1: 600 mg (oral) + 927 mg (SC) Day 2: 600 mg (oral) Days 1 and 2: 600 mg (oral), Day 8: 300 mg (oral), Day 15: 927 mg (SC) Day 1 to end of Month 6 Days 1 to 15 Day 15 to end of Month 6 CV = coefficient of variation; NA = not applicable; SC = subcutaneous C max (ng/mL) 101.4 (53.1) 88.0 (72.4) 86.5 (51.7) AUC tau (h∙ng/mL) 242266 (46.0) 19496 (72.6) 239163 (47.2) C trough (ng/mL) 32.5 (57.2) 46.9 (72.3) 32.5 (57.5) Lenacapavir…
🧬 Mechanism of Action ▾
12.1Mechanism of Action SUNLENCA is an HIV-1 antiretroviral agent [see Microbiology (12.4) ] .
📦 How Supplied / Storage and Handling ▾
16 HOW SUPPLIED/STORAGE AND HANDLING SUNLENCA tablets, 300 mg are beige, capsule-shaped, and film-coated with "GSI" debossed on one side and "62L" on the other side. SUNLENCA tablets are available in a bottle and blister packs, packaged as follows: Bottle SUNLENCA bottle contains 4 tablets (NDC 61958-3001-3). The bottle also contains a silica gel desiccant and polyester coil, and is closed with a child-resistant closure.
Do not remove the desiccant packet. Keep bottle tightly closed. Blister Packs SUNLENCA 4-Tablets™ blister pack contains 4 tablets (NDC 61958-3001-1) SUNLENCA 5-Tablets™ blister pack contains 5 tablets (NDC 61958-3001-2) Within the blister packs, tablets are packaged in a clear blister film sealed to a foil lidding material.
The blister card is fitted between two paperboard cards, and packaged with silica gel desiccant in a sealed child-resistant flexible laminated pouch. Store bottle and blister packs at 20 °C – 25 °C (68 °F – 77 °F), excursions permitted to 15 °C – 30 °C (59 °F – 86 °F) (see USP Controlled Room Temperature). Dispense and store only in original bottle or blister pack.
SUNLENCA injection is packaged in one of two different injection kits containing the following: Vial Access Device Injection Kit (NDC 61958-3002-1): 2 single-dose clear glass vials, each containing sufficient volume to allow withdrawal of 463.5 mg/1.5 mL (309 mg/mL) of lenacapavir. The injection solution is sterile, preservative-free, clear, and yellow with no visible particles. Vials are sealed with a stopper and aluminium overseal with flip-off cap.
2 vial access devices, 2 disposable syringes, and 2 injection safety needles for subcutaneous injection (22-gauge, ½ inch). Withdrawal Needle Injection Kit (NDC 61958-3005-1): 2 single-dose clear glass vials, each containing sufficient volume to allow withdrawal of 463.5 mg/1.5 mL (309 mg/mL) of lenacapavir. The injection solution is sterile, preservative-free, clear, and yellow with no visible particles.
Vials are sealed with a stopper and aluminium overseal with flip-off cap. 2 disposable syringes, 2 withdrawal needles (18-gauge, 1.5 inch; may be supplied with or without a safety shield), and 2 injection safety needles for subcutaneous injection (22-gauge, ½ inch). The vial stoppers are not made with natural rubber latex.
Store at 20 °C to 25 °C (68 °F to 77 °F), excursions permitted between 15 °C to 30 °C (59 °F to 86 °F). Keep the vials in the original carton until just prior to preparation of the injections in order to protect from light. Once the solution has been drawn into the syringes, the injections should be administered as soon as possible.
Discard any unused portion of the solution.
📦 Storage and Handling ▾
Store bottle and blister packs at 20 °C – 25 °C (68 °F – 77 °F), excursions permitted to 15 °C – 30 °C (59 °F – 86 °F) (see USP Controlled Room Temperature). Dispense and store only in original bottle or blister pack.
Store at 20 °C to 25 °C (68 °F to 77 °F), excursions permitted between 15 °C to 30 °C (59 °F to 86 °F). Keep the vials in the original carton until just prior to preparation of the injections in order to protect from light. Once the solution has been drawn into the syringes, the injections should be administered as soon as possible. Discard any unused portion of the solution.
📋 Description ▾
11 DESCRIPTION SUNLENCA tablets and SUNLENCA injection contain lenacapavir sodium, a capsid inhibitor. The chemical name of lenacapavir sodium is: Sodium (4-chloro-7-(2-(( S )-1-(2-((3b S ,4a R )-5,5-difluoro-3-(trifluoromethyl)-3b,4,4a,5-tetrahydro-1 H -cyclopropa[3,4]cyclopenta[1,2- c ]pyrazol-1-yl)acetamido)-2-(3,5-difluorophenyl)ethyl)-6-(3-methyl-3-(methylsulfonyl)but-1-yn-1-yl)pyridin-3-yl)-1-(2,2,2-trifluoroethyl)-1 H -indazol-3-yl)(methylsulfonyl)amide. Lenacapavir sodium has a molecular formula of C 39 H 31 ClF 10 N 7 NaO 5 S 2, a molecular weight of 990.3, and the following structural formula: Lenacapavir sodium is a light yellow to yellow solid and is practically insoluble in water.
Chemical Structure SUNLENCA tablets are for oral administration. Each film-coated tablet contains 300 mg of lenacapavir (present as 306.8 mg lenacapavir sodium) and the following inactive ingredients: copovidone, croscarmellose sodium, magnesium stearate, mannitol, microcrystalline cellulose, and poloxamer 407. The tablets are film-coated with a coating material containing iron oxide black, iron oxide red, iron oxide yellow, polyethylene glycol, polyvinyl alcohol, talc, and titanium dioxide.
SUNLENCA injection is for subcutaneous administration. Each single-dose vial contains 463.5 mg/1.5 mL (309 mg/mL) of lenacapavir (present as 473.1 mg/1.5 mL of lenacapavir sodium) as a sterile, preservative-free, clear, yellow solution and the following inactive ingredients: 896.3 mg of polyethylene glycol 300 (as solvent) and water for injection. The apparent pH range of the injection is 9.0–10.2.
The vial stoppers are not made with natural rubber latex.
💬 Information for Patients ▾
17 PATIENT COUNSELING INFORMATION Advise the patient to read the FDA-approved patient labeling (Patient Information). Drug Interactions SUNLENCA may interact with certain drugs; therefore, advise patients to report to their healthcare provider the use of any other prescription or non-prescription medication or herbal products, including St. John's wort, during treatment with SUNLENCA [see Contraindications (4) and Drug Interactions (7) ] .
If SUNLENCA is discontinued, advise patients that SUNLENCA may remain in the body and affect certain other drugs for up to 9 months after receiving their last injection [see Drug Interactions (7.2 , 7.3) ]. Immune Reconstitution Syndrome Advise patients to inform their healthcare provider immediately of any symptoms of infection, as in some patients with advanced HIV (AIDS), signs and symptoms of inflammation from previous infections may occur soon after anti-HIV treatment is started [see Warnings and Precautions (5.1) ] .
Adherence to SUNLENCA Counsel patients about the importance of continued medication adherence and scheduled visits to maintain viral suppression and to reduce risk of loss of virologic response and development of resistance. Advise patients to contact their healthcare provider immediately if they stop taking SUNLENCA or any other drug in their antiretroviral regimen [see Dosage and Administration (2.1) and Warnings and Precautions (5.2) ] . Missed Injection Dose: Treatment of HIV-1 in Heavily Treatment-Experienced Adults Inform patients that SUNLENCA can remain in the body for up to 12 months or longer after receiving their last injection.
Advise patients to contact their healthcare provider if they miss or plan to miss a scheduled injection visit and that oral SUNLENCA therapy may be used for up to 6 months to replace missed injections. Advise patients that oral dosing should be used on an interim basis only and that the maintenance injection dosage should be resumed at the earliest possible opportunity [see Dosage and Administration (2.2 , 2.4) and Warnings and Precautions (5.2) ] . Missed Oral Initiation Dose: Oral Loading for Initiation of BIXLENVO Inform patients that if they miss one of the two days of oral initiation doses of SUNLENCA given with BIXLENVO to take it as soon as possible [see Dosage and Administration (2.4) ].
Injection Site Reactions Inform patients that injection site reactions (ISRs), such as swelling, pain, erythema, nodule, induration, pruritus, extravasation or mass, may occur. Nodules and indurations at the injection site may take longer to resolve than other ISRs and may be persistent. Instruct patients when to contact their healthcare provider about these reactions [see Warnings and Precautions (5.3) ].
Pregnancy Registry Inform patients that there is an antiretroviral pregnancy registry to monitor fetal outcomes of pregnant individuals exposed to SUNLENCA [see Use in Specific Populations (8.1) ]. Lactation Inform individuals with HIV-1 that the potential risks of breastfeeding include: (1) HIV-1 transmission (in infants without HIV-1), (2) developing viral resistance (in infants with HIV), and (3) adverse reactions in a breastfed infant similar to those seen in adults [see Use in Specific Populations (8.2) ].