Generic Name

Opzelura (tirbanibulin)

Mechanism

Opzelura (tirbanibulin) is a selective inhibitor of Src‑family tyrosine kinases and the epidermal growth factor receptor (EGFR).
• Binds to the ATP‑binding pocket of Src, preventing phosphorylation of downstream targets.
• Blocks PI3K/Akt signaling, leading to apoptosis of HPV‑infected keratinocytes.
• Alters cytoskeletal dynamics, disrupting viral replication and spread.

Pharmacokinetics

• Route: Topical 1 % cream applied to the lesion.
• Absorption: Minimal systemic uptake; plasma levels < 1 ng mL⁻¹.
• Half‑life: Local skin residence ~4 days; systemic half‑life negligible.
• Metabolism & Excretion: Excreted unchanged via the skin; no significant hepatic or renal metabolism.
• Drug interactions: None reported due to negligible systemic exposure.

Indications

• Approved use: Treatment of genital warts (HPV 6/11) in adults.
• Regimen: Once‑daily application for 4 weeks.

Contraindications

• Contraindicated: Hypersensitivity to tirbanibulin or excipients.
• Cautions:
• May cause mild‑to‑moderate local irritation (erythema, pruritus).
• Avoid in active dermatitis, psoriasis, or eczematous lesions that could worsen.
• Pregnancy/Lactation: Not studied; use only if benefits outweigh risks.
• Children: Not indicated.

Dosing

• Apply 1 mL (≈ 1 g) of the cream to the entire eruption.
• Once daily, preferably at bedtime.
• Continue for 4 consecutive weeks or until complete clearance.
• Do not occlude the site; wash after 30 minutes if sweat is expected.

Adverse Effects

Common
• Local erythema (~30 %).
• Pruritus (~20 %).
• Mild burning/stinging on application.

Serious
• Rare severe dermatitis or drug‑reaction with eosinophilia and systemic symptoms (DRESS).
• No systemic toxicity reported.

Monitoring

• Clinical – Weekly inspection of lesions for clearance or progression.
• Dermatologic – Watch for signs of excessive inflammation; discontinue if severe erythema or ulceration appears.
• Patient education – Report fever or malaise immediately.
• Lab tests – None required.

Clinical Pearls

• Skin prep matters: Use fragrance‑free cleansers before application to lessen irritation.
• Avoid overlapping topicals: Do not use other immunomodulators concurrently on the same area.
• Gentle wiping: Lightly pat the treated area with gauze before re‑applying to prevent drug buildup.
• Early response: Significant improvement often noted by week 2, encouraging patient adherence.
• Results vs placebo: Phase III trials showed 71 % complete clearance versus 3 % for placebo.
• Broad‑spectrum applicability: Works on warts refractory to cryotherapy or salicylic acid, independent of viral load.

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