Axitinib
Deterministic view of the source YAML entity. Clinical authority remains with the cited source IDs and reviewer sign-off state.
| ID | DRUG-AXITINIB |
|---|---|
| Type | Drug |
| Aliases | AG-013736InlytaАкситиніб |
| Status | reviewed 2026-04-27 | pending_clinical_signoff |
| Diseases | DIS-RCC |
| Sources | SRC-ESMO-RCC-2024 SRC-NCCN-KIDNEY-2025 |
Drug Facts
| Class | Selective VEGFR-1/2/3 tyrosine kinase inhibitor (2nd-generation) |
|---|---|
| Mechanism | Selective ATP-competitive small-molecule TKI of VEGFR-1, VEGFR-2, and VEGFR-3 with sub-nanomolar in-vitro potency and improved selectivity over first-generation multikinase TKIs (sunitinib, sorafenib). Blocks VEGF-driven endothelial proliferation, migration, and survival in the tumor microenvironment, producing predominantly anti-angiogenic effects with minimal direct cytotoxicity. Short half-life (~2.5-6 h) gives titratable BID dosing — characteristic patient-specific dose escalation based on blood-pressure response (titrate up to 10 mg BID if BP tolerable at 5 mg). Pivotal evidence: AXIS (axitinib vs sorafenib 2L mRCC post-sunitinib/cytokines: mPFS 6.7 vs 4.7 mo); KEYNOTE-426 (pembrolizumab + axitinib vs sunitinib 1L mRCC: mPFS 15.7 vs 11.1 mo, OS HR 0.53), JAVELIN Renal 101 (avelumab + axitinib vs sunitinib 1L mRCC). |
| Typical dosing | Starting dose: 5 mg PO BID (~12 h apart), with or without food. Titration: if BP normal/well-controlled and no G≥2 AE for ≥2 consecutive weeks → escalate to 7 mg BID, then to 10 mg BID similarly. Dose level -1 = 3 mg BID; -2 = 2 mg BID; permanent discontinuation if recurrent G3-4 at -2. Hold for hypertensive crisis, severe HFS, severe proteinuria, GI perforation, or hemorrhage. Strong CYP3A4 inhibitor coadministration: halve starting dose to 2 mg BID. No formal renal adjustment for CrCl ≥30; modest adjustment in moderate hepatic impairment (50% dose reduction recommended for Child-Pugh B). |
| Ukraine registered | True |
| NSZU reimbursed | True |
| Ukraine last verified | 2026-04-27 |
Notes
Patient-specific titration to maximum tolerated dose (5 → 7 → 10 mg BID) is a defining feature — patients tolerating starting dose with normotension should escalate, as exposure correlates with efficacy. KEYNOTE-426 + JAVELIN-Renal-101 redefined 1L mRCC by combining axitinib with anti-PD-(L)1 — dual mechanism of action outperforms sunitinib monotherapy. Baseline workup: BP, urinalysis (UPCR), LFTs, CBC, TSH, ECG, pregnancy test. Monitor BP weekly first 6 weeks then monthly, urinalysis monthly, LFTs monthly, TSH q3 months. Hold for SBP >160/100 — escalate antihypertensives (ACE-i / ARB first then CCB amlodipine). Hold ≥2 weeks before elective surgery; resume only after full wound healing. Counsel patients on dental procedures (bleeding risk). UA: registered; НСЗУ-reimbursed in RCC.
Used By
Regimens
REG-PEMBRO-AXI-RCC- Pembrolizumab + axitinib (RCC, 1L all-risk)