Pralsetinib
Deterministic view of the source YAML entity. Clinical authority remains with the cited source IDs and reviewer sign-off state.
| ID | DRUG-PRALSETINIB |
|---|---|
| Type | Drug |
| Aliases | BLU-667GavretoПралсетініб |
| Status | reviewed 2026-04-27 | pending_clinical_signoff |
| Diseases | None declared |
| Sources | SRC-ESMO-NSCLC-METASTATIC-2024 SRC-NCCN-NSCLC-2025 |
Drug Facts
| Class | Selective RET tyrosine kinase inhibitor |
|---|---|
| Mechanism | Highly selective ATP-competitive small-molecule inhibitor of the RET (REarranged during Transfection) receptor tyrosine kinase, active against RET fusions (KIF5B-RET, CCDC6-RET dominant in NSCLC; diverse fusions in papillary thyroid) and RET-activating point mutations including M918T (germline / sporadic medullary thyroid carcinoma). Designed for selectivity vs VEGFR2 to spare class VEGFR-mediated cardiovascular toxicity (although hypertension still occurs). CNS-penetrant. Pivotal trials ARROW: RET-fusion+ NSCLC TKI-naive ORR ~70%, prior platinum ORR ~57%; RET-mutant medullary thyroid ORR ~60%; RET-fusion+ thyroid (papillary, anaplastic) ORR ~89%. FDA approved Sep 2020. Note commercial availability has contracted in 2023-2024 — Roche returned US rights to Blueprint; some indications were withdrawn from US label while EU access continues; selpercatinib is the more widely available RET-TK... |
| Typical dosing | 400 mg PO once daily on an empty stomach (no food 2 h before, 1 h after — fed-state increases exposure ~100%, raising AE risk). Continuous until progression / unacceptable toxicity. Dose level -1 = 300 mg daily; -2 = 200 mg daily; -3 = 100 mg daily; permanent discontinuation if recurrent G3-4 at -3. Hold for ILD/pneumonitis (any grade — workup, permanently discontinue if confirmed), hypertensive crisis, severe hepatotoxicity. No formal renal adjustment. |
| Ukraine registered | False |
| NSZU reimbursed | False |
| Ukraine last verified | 2026-04-27 |
Notes
Same RET-TKI class as selpercatinib; LIBRETTO-431 head-to-head (selpercatinib vs platinum + pembrolizumab in RET+ NSCLC 1L) established selpercatinib as preferred where access permits. Critical fasting administration (high-fat meal nearly doubles AUC). Baseline + ongoing monitoring: BP weekly first month then monthly, CBC q2 wk first 2 mo then monthly, LFTs q2 wk first 8 wk then monthly, ECG (QTc) baseline + periodic, CT chest at any new respiratory symptoms. Hold for elective surgery ≥1 week pre and resume only after full wound healing. In contemporary US practice some pralsetinib indications have been withdrawn (Roche → Blueprint hand-back); EU and EAP access continues. UA: not registered; pursue selpercatinib EAP first if RET+ tumor and access pathway available.
Used By
No reverse references found in the YAML corpus.