cabotegravir (Rx)

Brand and Other Names:Vocabria
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Dosing & Uses

AdultPediatric

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

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Interactions

Interaction Checker

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            Adverse Effects

            <1%

            Headache

            Nausea

            Abnormal dreams

            Anxiety

            Insomnia

            Frequency Not Defined

            Hypersensitivity

            Hepatotoxicity

            Depressive disorders

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            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
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            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.

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            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%

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            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)

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            Formulary

            FormularyPatient Discounts

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            The above information is provided for general informational and educational purposes only. Individual plans may vary and formulary information changes. Contact the applicable plan provider for the most current information.

            Tier Description
            1 This drug is available at the lowest co-pay. Most commonly, these are generic drugs.
            2 This drug is available at a middle level co-pay. Most commonly, these are "preferred" (on formulary) brand drugs.
            3 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs.
            4 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            5 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
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            NC NOT COVERED – Drugs that are not covered by the plan.
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            Medscape prescription drug monographs are based on FDA-approved labeling information, unless otherwise noted, combined with additional data derived from primary medical literature.