Sunlenca
There are two initiation dosing schedules, both consisting of a combination of lenacapavir tablets and subcutaneous injections. The first consists of the two subcutaneous injections + 600 mg oral LEN (two 300 mg tablets) on Day 1 and 600 mg oral LEN on Day 2. The second consists of 600 mg oral LEN on Day 1 and Day 2, 300 mg on Day 8 and the two injections on Day 15. The first maintenance dose begins six months later, give or take two weeks. If more than 28 weeks pass without the maintenance dose, restart therapy with initiation dosing followed by the maintenance dose six months later.
Currently, no dosage adjustment is recommended in patients with mild, moderate or severe renal impairment; however, Sunlenca has not been studied in people who have end stage renal disease with a CrCl less than 15mL/min. No dosage adjustment is recommended for people with mild or moderate hepatic (liver) impairment. Sunlenca has not been studied in people with severe hepatic impairment (Child-Pugh Class C).
- See package insert for more complete information on potential side effects and interactions.
gilead.com; sunlenca.com
(800) GILEAD-5 (445-3235)
JO-ANN JOSE, MD, MPH:
Sunlenca—lenacapavir—is an effective and genetically fragile compound. It is administered as one shot in the butt twice yearly—every six months. This medication is for people who are highly treatment-experienced and may have few other treatment options open to them; it is taken to supplement the oral regimen (background therapy) that a person is already taking. We are talking about people who have had a significant history of HIV, whose virus has developed mutations making it resistant to other drugs and drug classes. The individual has to have an optimized background regimen that they are highly adherent to, and then we add the lenacapavir on top of that. Because lenacapavir is a long-acting injectable, it has the potential to stay in your system up to nine months after your last shot. This long half-life means that there is a potential for drug-drug interactions and resistance mutation development. Adherence is very important. It is a very expensive drug, so if you need to use Sunlenca, there is going to be a prior authorization process with your insurance company. It might take a little bit of time for you and your care provider’s office to go through that process, so don’t get frustrated. It is very exciting that we have this as an option, especially for people who are highly treatment experienced, who may not have a lot of other options.
Do not take with carbamazepine, eslicarbazepine, oxcarbazepine, phenobarbital or phenytoin; rifampin, rifabutin or rifapentine; pimozide; amiodarone, disopyramide, quinidine, bosentan, ivabradine, lomitapide, cisapride, flibanserin or St. John’s wort. Start the following medications at the lowest dose, titrate carefully and monitor for safety--dexamethasone (do not take more than 16mg/day), hydrocortisone or cortisone and lovastatin or simvastatin. Not recommended with ergot derivatives (dihydroergotamine, ergotamine and methylergonovine) or tadalafil (for pulmonary arterial hypertension, or PAH). See package insert for dose recommendations with erectile dysfunction drugs sildenafil and vardenafil. Dose adjustment may be needed for buprenorphine or methadone; start these medications by titrating to desired effect but use lowest feasible doses for initiation or maintenance and monitor effects. Co-administration with immunosuppressants such as cyclosporine, everolimus, sirolimus or tacrolimus will require a dose adjustment for these medications and careful monitoring and dose titration based on drug levels—must be monitored very closely. Carefully monitor the effects of fentanyl and oxycodone; tramadol dose may need to be decreased. Avoid naloxegol (for opioid-induced constipation); if unavoidable, decrease its dose and monitor for adverse reactions. Use with caution with alfuzosin; if co-administration is necessary, monitor blood pressure closely and titrate dose of alfuzosin. Avoid use with beaquiline or quetiapine if possible; if benefits outweigh risks for coadministration, monitor liver function and ECG for QTc prolongation. Use caution with triazolam and oral midazolam (Versed). Use with caution if co-administering with warfarin; monitor INR and titrate warfarin dose as clinically indicated. If giving with the psych medications buspirone, paroxetine, brexpiprazole, iloperidone, lumateperone, lurasidone or trazodone, monitor for side effects and may need to use lower dose of psych medication. Avoid use with clopidogrel but if co-administration is required, monitor for clopidogrel adverse effects. Try to avoid co-administration with lidocaine, propafenone, dronedarone, diltiazem, verapamil and digoxin, but if necessary, monitor closely for adverse effects. Use with caution if co-administering with eplerenone or ranolazine; a dose adjustment of these meds will be necessary if taken at same time as Sunlenca. Use caution if co-administering with colchicine used for gout--it will require a dose adjustment and monitoring of colchicine. Okay to take with the cholesterol drug rosuvastatin (Crestor), tenofovir alafenamide (TAF, found in Descovy and other medications), tenofovir DF (TDF, found in Truvada and other medications), HCV medications and the antifungal voriconazole. Certain HIV medications cannot be given with Sunlenca because a drug interaction will render it ineffective: do not co-administer with efavirenz, etravirine, nevirapine or boosted or unboosted atazanavir; these medications are rarely prescribed today. Tell your provider or pharmacist about all medications, herbals and supplements you are taking or thinking of taking, prescribed or not, as there may be other drug interactions which are not listed here.
Injection site reactions (generally considered mild and transient), nodules (bumps) and indurations (skin thickening). In the CAPELLA study, for Grade 3 and 4 laboratory abnormalities, 5% of participants experienced high blood sugar, 6% experienced excess sugar in urine and 13% experienced low creatinine clearance (eGFR) or high serum creatinine. These observed changes were related to the individual’s diabetes or were either transient or unconfirmed. Nausea occurred in 4% of participants.
Sunlenca is the first in its drug class. It is highly potent at low doses. Drug efficacy was similar across demographic groups (race, sex at birth, age and geographic region), CD4 cell count and viral load at study entry and which background HIV medications were used. Sunlenca thwarts HIV by interfering with multiple essential steps of the viral lifecycle. Ultimately, it prevents viral RNA from entering the nucleus of human CD4 T cells, halting virus assembly and protein formation and inhibiting assembly of new viral particles. At this time, there are insufficient data to support the initiation of Sunlenca during pregnancy. People who become pregnant while on Sunlenca do not necessarily have to switch to another regimen, but may undergo closer monitoring of viral load. Pregnant individuals can voluntarily enroll in the Antiretroviral Pregnancy Registry through their provider; GO TO apregistry.com.
JUAN MICHAEL PORTER II:
Sunlenca is lenacapavir (LEN) for HIV treatment. It’s an injectable that is only available for people who are currently on treatment. But Carl Dieffenbach, PhD, told me that with the success of lenacapavir for HIV prevention, needing treatment every six months will become the new standard not only for injectables but for oral pills as well. There have been some questions about possible resistance to LEN, though Weill Cornell Medicine (formerly Cornell University Medical College) just released data from a study in Uganda showing few incidents among people who are treatment-naïve.