Rukobia
Take missed dose as soon as possible, as long as it is at least 12 hours before your next dose. Do not double up on your next dose. Tablet should be swallowed whole; do not chew, crush or split tablets.
- See package insert for more complete information on potential side effects and interactions.
viivhealthcare.com; rukobia.com
(877) 844-8872
JO-ANN JOSE, MD, MPH:
Fostemsavir is approved only for people who are very treatment-experienced and have significant resistance mutations that preclude the use of other medications. It has to be taken twice daily and is generally well tolerated. Rukobia is an oral option for heavily treatment-experienced people as opposed to an injectable like lenacapavir or cabotegravir. There are some medication interactions that are important to know, including with some hepatitis C medicines, some oral contraceptives and many of the statin drugs, which are used to treat high cholesterol or prevent cardiovascular complications. Before you start this medicine, you and your doctor should discuss drug interactions extensively. It is not studied in pregnancy. There are insufficient data, so it cannot be used in pregnancy. As an entry attachment inhibitor, Rukobia is part of a relatively new class of drugs. It has a high price tag, so there’s often an extensive prior authorization process with your insurance company to get it covered. That doesn’t mean that you shouldn’t or can’t access it. If you are on a very expensive HIV regimen, before you change insurance plans, it’s important to make sure that the new plan will continue to provide coverage of that medicine.
Dose modification of fostemsavir is not required when co-administering with atazanavir/ritonavir (Reyataz + Norvir), cobicistat (Tybost), darunavir/cobicistat (Prezcobix), darunavir/ritonavir (Prezista + Norvir) with and without etravirine (Intelence), maraviroc (Selzentry), raltegravir (Isentress HD), ritonavir, ibalizumab (Trogarzo), lenacapavir (Sunlenca) or tenofovir DF (found in Truvada). Dose modification is also not required when co-administering with buprenorphine/naloxone, famotidine, methadone, norethindrone or rifabutin (with or without ritonavir). It is not recommended to co-administer with rifampin or rifapentine, antimycobacterial drugs used for tuberculosis treatment, due to significantly reduced levels of fostemsavir. Cannot be taken with (contraindicated with) enzalutamide (an androgen receptor inhibitor), the anticonvulsants carbamazepine, phenobarbital and phenytoin, the cancer drug mitotane or the herb St. John’s wort. Fostemsavir increases concentrations of statins (medications that treat cholesterol). Use the lowest possible starting dose for statins and monitor for statin-associated adverse effects. Rukobia should be used with caution when taken with other medications known to have a risk for torsades de pointes or QT prolongation (these abnormal heart rhythms can make the heart stop). Fostemsavir could affect oral contraceptive concentrations, especially those containing ethinyl estradiol. If a booster is not given in the regimen with fostemsavir, it may be co-administered with a combined oral contraceptive containing norethindrone and 30 mcg or less of ethinyl estradiol. It cannot be taken by trans women on estrogen hormone therapy due to the significantly increased risk for a blood clot. May increase levels of the hepatitis C (HCV) drugs grazoprevir and voxilaprevir; however, the magnitude of increase in exposure is currently unknown. Increased levels of grazoprevir may increase the risk of elevated liver enzyme levels. Use an alternative HCV regimen if possible. 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.
The most common side effect is nausea in 10% of study participants. Other side effects, observed less often, were diarrhea, fatigue and headache. Use with caution in people who have a history of QTc prolongation (these abnormal heart rhythms can make the heart stop). Liver problems can occur but are very rare. The risk may be greater for people with a history of hepatitis B or C, but may occur in people without a history of liver disease. Clinically relevant increases in serum creatinine have occurred in patients taking Rukobia who have risk factors for reduced renal (kidney) function (including pre-existing history of renal disease and/or taking other medications at the same time that are known to cause increases in creatinine). A causal relationship between Rukobia and increased serum creatinine has not been established. Increases in direct bilirubin have also been observed. Cases of clinical significance were uncommon and were typically transient, occurred without increases in liver enzymes and resolved on continued Rukobia therapy.
Rukobia is designed to be used in highly treatment-experienced people who typically have fewer options for HIV treatment than individuals who are new to antiretroviral therapy. An option for treatment-experienced individuals is a good thing. “Even in the era of modern HAART [highly active antiretroviral therapy], antiretroviral [ARV] failure and resistance is still a problem worldwide,” wrote HIV specialist Pedro Cahn, MD, PhD, and colleagues in Current Opinion in HIV and AIDS published July 2018. Dr. Cahn worked on fostemsavir research. Rukobia is a gp120 attachment inhibitor. A member of the drug class of HIV entry inhibitors, Rukobia works on the gp120 envelope protein that lies on the surface of the virus. It’s a necessary part of getting the virus to enter the cell. Rukobia prevents attachment to the CD4 immune cell by blocking gp120 from binding to the CD4 receptor binding sites. Watch a video of its mechanism of action at youtu.be/WnreXE-TVi8. Given that Rukobia does not appear to have cross-resistance to any currently approved antiretroviral, as well as its activity regardless of HIV tropism, it is a welcome option for people with very limited choices for treatment. Rukobia is active against CCR5, CXCR4 and dual-mixed virus; Selzentry is only active against CCR5. For individuals with HIV-2, primarily found in West Africa but also present in other countries, Rukobia would not be recommended, as HIV-2 is inherently resistant to it. For more data, including medications added for optimized therapy. GO TO the FDA approval announcement at fda.gov/news-events/press-announcements/fda-approves-new-hiv-treatment-patients-limited-treatment-options. Pregnant individuals can voluntarily enroll in the Antiretroviral Pregnancy Registry through their provider; GO TO apregistry.com.
JUAN MICHAEL PORTER II:
No one is using Rukobia as their first treatment option. It’s specifically for people who’ve been in treatment for a long time and—because of virologic failure—don’t have many other treatment options. Rukobia is made up of fostemsavir, which makes it unsuitable for treating HIV-2 (seen primarily in West Africa and in other countries), because that strain of the virus is resistant to the drug.