Generic Name

Cabenuva

Mechanism

• Cabotegravir: binds covalently to the integrase catalytic core domain, blocking strand‑transfer and preventing viral DNA integration into the host genome.
• Rilpivirine: allosterically binds to the reverse transcriptase active site, inhibiting the conversion of viral RNA to DNA.
• The dual‑mechanism design reduces the likelihood of resistance and enhances potency when both agents are present at therapeutic concentrations.

Pharmacokinetics

• Dose‑dependent pharmacokinetics: Higher plasma concentrations after initial oral lead‑in improve injection‑site absorption.
• Stable levels: Reaching a steady state after ~3 bi‑weekly injections.

Indications

• Treatment of HIV‑1 infection in adults who are:
• Antiretroviral (ARV)‑naïve or
• Virologically suppressed on a stable regimen for at least 6 months.
• Prescription requires prior oral lead‑in: 800 mg cabotegravir/600 mg rilpivirine PO q4 weeks for 4 weeks.

Contraindications

• Contraindicated in patients with:
• Known hypersensitivity to cabotegravir, rilpivirine, or excipients.
• Warnings:
• Injection‑site reactions: pain, erythema, abscess, induration.
• Drug‑drug interactions: potent CYP3A4 or UGT1A1 inducers (e.g., carbamazepine, phenytoin) diminish drug levels; potent inhibitors (e.g., ritonavir) may increase exposure.
• CNS effects: dizziness, insomnia; caution with alcohol or CNS depressants.
• Hepatotoxicity: rare; monitor LFTs baseline and at month 1, 3, and 6.
• Emergent resistance: discontinuation or errors in scheduling may select for integrase or reverse‑transcriptase mutants; consider rescue therapy if adherence lapses.

Dosing

1. Oral lead‑in (4 weeks)
• Cabotegravir 800 mg + Rilpivirine 600 mg PO QD
• Continue for 4 weeks to establish serum levels.

2. Injectable maintenance (every 8 weeks)
• Cabotegravir 600 mg + Rilpivirine 200 mg IM (deltoid/supragluteal)
• Dose volume: 3 mL (mix sterile water); utilize a single‑use auto‑injector.

3. Missed dose: if >3 weeks late, resume oral lead‑in before next injection.

Adverse Effects

• Common (≥5 %):
• Injection‑site pain, erythema, swelling
• Headache, insomnia, nausea, fatigue
• Arthralgia, myalgia
• Serious (≤1 %):
• Severe hypersensitivity rash (Stevens–Johnson syndrome)
• Hepatotoxicity (ALT/AST >5× ULN)
• Central nervous system depression (rare)
• Injection‑site abscess requiring incision/drainage

Monitoring

• Baseline: CBC, CMP, viral load (VL), CD4 count, hepatitis serologies, renal function.
• Follow‑up:
• VL & CD4 at 4 weeks after first injection, then every 6 months.
• LFTs & kidney function at 3 months, then annually.
• Injection‑site assessment at each visit.
• Check for signs of drug resistance if VL >200 copies/mL.

Clinical Pearls

• Patient selection: Ideal for those with excellent adherence, low risk of missing injections, and no active infections that could impair absorption.
• Injection technique: Use a 1/4‑inch needle; rotate sites (deltoid or gluteal) to reduce lipodystrophy; observe for talskin or local hematoma.
• Lead‑in importance: Skipping or shortening the oral lead‑in significantly increases the risk of virologic failure and resistance.
• Drug interactions: Prioritize a comprehensive medication review to identify CYP3A4/UGT1A1 modifiers; consider dose adjustments for ritonavir‑boosted protease inhibitors.
• Pregnancy: Cabotegravir is category C; limited data on rilpivirine; weigh benefits vs. risks, consider continued daily oral regimen if essential.
• Switching strategy: When transitioning from daily oral therapy, ensure >1 month of viral suppression before initiating bi‑weekly injections to mitigate the risk of emergent therapy resistance.

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