Dosing & Uses
Dosage Forms & Strengths
tablet
- 30mg
HIV Infection
Indicated in combination with rilpivirine PO as a complete regimen for short-term treatment of human immunodeficiency virus type 1 (HIV-1) infection in adults who are virologically suppressed (HIV-1 RNA <50 copies/mL) on a stable antiretroviral therapy (ART) regimen with no history of treatment failure and with no known or suspected resistance to either cabotegravir or rilpivirine
Indication specifics
- Oral lead-in to assess tolerability of cabotegravir before administration of cabotegravir extended-release injectable IM suspension, a component of Cabenuva (cabotegravir; rilpivirine extended-release injectable suspensions)
- Oral therapy for patients who will miss planned IM injection dosing with cabotegravir
Oral lead-in dosing prior to Cabenuva
- 30 mg PO qDay plus rilpivirine 25 mg PO qDay for at least 28 days
- Take last oral dose on the same day injections with Cabenuva are started
Oral replacement dose for planned missed Cabenuva injections
- If patient plans to miss scheduled Cabenuva (cabotegravir; rilpivirine) ER injectable suspensions by >7 days, take daily PO therapy to replace up to 2 consecutive monthly injection visits
- 30 mg PO qDay plus rilpivirine 25 mg PO qDay as replacement for up to 2 consecutive months
- Take first oral dose ~1 month after the last injection of Cabenuva and continue until the day injection dosing restarted
Dosage Modifications
Renal impairment
- Mild-to-severe (CrCl <90 mL/min): No dosage adjustment required
- ESRD (<15 mL/min): Pharmacokinetic effects are unknown
- Dialysis: Cabotegravir is >99% protein bound; dialysis is not expected to alter systemic exposure
Hepatic impairment
- Mild or moderate (Child-Pugh A or B): No dosage adjustment required
- Severe (Child-Pugh C): Pharmacokinetic effects are unknown
Safety and efficacy not established
Interactions
Interaction Checker
No Results

Contraindicated
Serious - Use Alternative
Significant - Monitor Closely
Minor

Adverse Effects
<1%
Headache
Nausea
Abnormal dreams
Anxiety
Insomnia
Frequency Not Defined
Hypersensitivity
Hepatotoxicity
Depressive disorders
Warnings
Contraindications
Documented hypersensitivity
Coadministration with UGT1A1/1A9 inducers such as carbamazepine, oxcarbazepine, phenobarbital, phenytoin, rifampin, and rifapentine, owing to possible loss of virologic response
Note: Use of Cabenuva ER injectable suspensions with rifabutin is contraindicated
Cautions
Hepatotoxicity reported in patients with or without known preexisting hepatic disease or known risk factors; monitoring of liver chemistries recommended; discontinue treatment if hepatotoxicity suspected
Depressive disorders (including depressed mood, depression, mood altered, mood swings) reported; promptly evaluate if symptoms emerge; determine whether risks of continued therapy outweigh benefits
Owing to use in combination with rilpivirine, consider contraindications, cautions, and drug interactions associated with rilpivirine
Hypersensitivity
- Serious or severe hypersensitivity reactions reported with other integrase inhibitors
- Discontinue immediately if signs or symptoms of hypersensitivity reactions develop (including, but not limited to, severe rash, or rash accompanied by fever, general malaise, fatigue, muscle or joint aches, blisters, mucosal involvement [oral blisters or lesions], conjunctivitis, facial edema, hepatitis, eosinophilia, angioedema, difficulty breathing)
- Monitor clinical status, including liver transaminases, and initiate appropriate therapy as warranted
Drug interaction overview
-
Other antiretroviral medications for HIV-1 infection
- Cabotegravir plus rilpivirine is a complete ART regimen
- Coadministration with other ARTs is not recommended
-
UGT1A1 or UGT1A9 inducers
- Contraindicated
- Primarily metabolized by UGT1A1 with some contribution from UGT1A9
- Strong UGT1A1 or 1A9 inducers are expected to decrease cabotegravir plasma concentrations and may result in loss of virologic response
-
Polyvalent cation-containing products
- Modify dosage schedule
- Coadministration with antacids containing polyvalent cations (eg, aluminum, magnesium hydroxide, calcium carbonate) may decrease cabotegravir absorption
- Administer antacids at least 2 hr before or 4 hr after taking cabotegravir
Pregnancy & Lactation
Pregnancy
Healthcare providers are encouraged to register patients by calling the Antiretroviral Pregnancy Registry (APR) 1-800-258-4263
Data are insufficient regarding use during pregnancy to adequately assess drug-associated risk of birth defects and miscarriage
While there are insufficient human data to assess the risk of neural tube defects (NTDs) with exposure to cabotegravir during pregnancy, NTDs were associated with dolutegravir, another integrase inhibitor
Lactation
Unknown if present in human breast milk, affects human milk production, or effects on breastfed infants
CDC recommends that females in the United States should not breastfeed their infants because of risk of the following
- Postnatal HIV transmission (in HIV-negative infants)
- Developing viral resistance (in HIV-positive infants)
- Adverse reactions in nursing infants
Animal data
- Animal lactation studies have not been conducted; however, cabotegravir was detected in plasma of nursing pups on lactation day 10 in rat prenatal and postnatal development study
Pregnancy Categories
A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk. C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done. D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk. X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist. NA: Information not available.Pharmacology
Mechanism of Action
Inhibits HIV integrase by binding to the integrase-active site and blocking the strand transfer step of retroviral DNA integration, which is essential for the HIV replication cycle
Absorption
Peak plasma time: 3 hr
Peak plasma concentration: 8 mcg/mL
AUC: 145 mcg⋅h/mL
Distribution
Protein bound: >99.8%
Metabolism
Metabolized by UGT1A1 (major) and UGT1A9 (minor)
Elimination
Half-life: 41 hr
Excretion: Urine 27%; feces 59%
Administration
Oral Administration
Take on regular dosing schedule with a meal at the same time as rilpivirine
Missed dose: Take as soon as remembered
Do not stop taking the drug or run out of cabotegravir, owing risk for viral resistance
Storage
Store below 30ºC (86ºF)
Images
Patient Handout
Formulary
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