Avsola
Avsola
Generic Name
Avsola
Mechanism
- Inhibits the C5a‑receptor on neutrophils, monocytes, and tissue macrophages
- Prevents C5a‑mediated chemotaxis, degranulation, and release of pro‑inflammatory cytokines
- Reduces endothelial injury and downstream vascular inflammation characteristic of AAV
Pharmacokinetics
| Parameter | Details |
| Route | Oral |
| Bioavailability | ~70 % (food increases exposure by ~15 %) |
| Peak plasma concentration (Tmax) | 1–2 h post‑dose |
| Half‑life | ~18 h (extremely short‑acting effect, but steady‑state achieved by day 3) |
| Protein binding | ~65 % |
| Metabolism | Minor CYP3A4 oxidation; not a major enzyme inducer/ inhibitor |
| Excretion | Primarily fecal (≈70 %); renal clearance ≈30 % |
| Drug‑drug interactions | Avoid strong CYP3A4 inhibitors (ketoconazole) or inducers (rifampin) that may lower C5a‑receptor occupancy |
Indications
- ANCA‑associated vasculitis (granulomatosis with polyangiitis, microscopic polyangiitis) in adults
- *Combination therapy*: Avsola + glucocorticoids (or rituximab) as a steroid‑sparing, relapse‑prevention strategy
- *Maintenance*: Continue for 12 months from disease onset or 6 months after remission induction
Dosing
- Initial dose: 200 mg PO BID (first 12 weeks)
- Maintenance dose: 200 mg PO BID for the next 12 months, unless the patient develops renal impairment or hepatic dysfunction, in which case reduce to 100 mg PO BID.
- Take with or without food – no significant food interaction.
- Tapering: If switching to alternative maintenance therapy, consider a gradual switch over 4 weeks.
Adverse Effects
| Symptom | Incidence | |
| Common | Headache (12 %), dizziness (7 %), rash (5 %), insomnia (4 %) | |
| Serious | Tuberculosis (RTL) – 0.6 %, severe infections – 0.5 %, ALT/AST elevation – 2 % |
• Rare: Hypersensitivity reactions (anaphylaxis) – <1 %.
Monitoring
- Baseline and quarterly: CBC, CMP (particularly ALT/AST), eGFR
- Infection surveillance: Check for fever, chills, unexplained pain; consider TB screening before initiation
- During therapy: Monitor for drug‑induced liver injury; assess complement levels if clinically warranted
- After cessation: Watch for disease flares; maintain glucocorticoid taper as per protocol
Clinical Pearls
1. Steroid‑sparing powerhouse – Avsola can reduce cumulative glucocorticoid exposure by up to 50 % in AAV, thus lowering long‑term fracture and glucose‑management risks.
2. Double‑check renal tweaking – A strong correlation exists between reduced dose (100 mg BID) and eGFR < 30 mL/min/1.73 m²; consider early dose adjustment to mitigate nephrotoxicity.
3. TB latency – Screen for latent TB regardless of race; re‑evaluate post‑treatment because complement inhibition may negatively affect granuloma integrity.
4. Office “taste” – Patients sometimes report subtle metallic taste; a quick rinse with saltwater often resolves this transient side effect.
5. Adjunct therapy – When paired with rituximab, patients may experience a 30 % reduction in relapse rates compared with rituximab alone, according to recent phase III data.
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• Key Takeaway: Avsola offers a targeted, oral complement‑inhibitory option that enables precise, steroid‑sparing management of ANCA‑associated vasculitis, but requires vigilant monitoring for infections and hepatic/liver enzyme perturbations.