Pemetrexed
Детермінований перегляд YAML-сутності з джерельної бази. Клінічний авторитет лишається за вказаними source ID та статусом клінічного sign-off.
| ID | DRUG-PEMETREXED |
|---|---|
| Тип | Препарат |
| Синоніми | AlimtaLY231514MTAПеметрексед |
| Статус | переглянуто 2026-04-27 | очікує клінічного підпису |
| Хвороби | DIS-MESOTHELIOMA DIS-NSCLC |
| Джерела | SRC-ESMO-NSCLC-METASTATIC-2024 SRC-NCCN-NSCLC-2025 |
Дані про препарат
| Клас | Multi-targeted antifolate antimetabolite |
|---|---|
| Механізм дії | Pyrrolopyrimidine antifolate that, after intracellular polyglutamation by folylpolyglutamate synthetase, simultaneously inhibits multiple folate-dependent enzymes critical for thymidine and purine biosynthesis: thymidylate synthase (TS — primary target), dihydrofolate reductase (DHFR), and glycinamide ribonucleotide formyltransferase (GARFT). The combined inhibition disrupts both thymidylate and purine de-novo synthesis, halting DNA / RNA production and producing S-phase-specific cytotoxicity. Activity is histology-restricted: highly active in non-squamous NSCLC and malignant pleural mesothelioma (MPM); minimal-to-no activity in squamous NSCLC due to higher baseline TS expression in squamous histology. Mandatory folic acid (vitamin B9) and vitamin B12 supplementation reduce hematologic and mucosal toxicity by ~50% without compromising efficacy (Niyikiza 2002, Vogelzang EMPHACIS). Backbo... |
| Типове дозування | Standard: 500 mg/m² IV over 10 minutes every 21 days. Combinations: + cisplatin 75 mg/m² IV Day 1 (mesothelioma EMPHACIS, NSCLC AVAPERL); + carboplatin AUC 5-6 IV Day 1 (NSCLC alternative); + pembrolizumab 200 mg IV q3w (KEYNOTE-189). Maintenance after induction: 500 mg/m² q3w continuing until progression. CRITICAL pre-medication regimen to mitigate hematologic and mucosal toxicity: folic acid 350-1000 mcg PO daily starting ≥7 days before first pemetrexed dose, continuing throughout treatment and 3 weeks post; vitamin B12 1000 mcg IM ≥7 days before first dose then every 9 weeks throughout treatment; dexamethasone 4 mg PO BID Days 0, 1, 2 of each cycle (rash prophylaxis). Renal adjustment: a... |
| Зареєстровано в Україні | True |
| Відшкодовується НСЗУ | True |
| Остання перевірка для України | 2026-04-27 |
Нотатки
Standard backbone for non-squamous NSCLC (KEYNOTE-189: carbo + pem + pembro vs carbo + pem placebo, OS HR 0.49 in PD-L1-all- comers — practice-defining 1L for non-squamous EGFR/ALK-WT NSCLC) and for malignant pleural mesothelioma (EMPHACIS cis + pem mOS 12.1 vs 9.3 mo — historical 1L until CheckMate-743 added nivo+ipi as combo option). NOT active in squamous NSCLC — histology- specific selection is critical. Mandatory pre-medication: folic acid 350-1000 mcg PO daily (start ≥7 days pre-cycle 1), B12 1000 mcg IM (start ≥7 days pre-cycle 1, then q9 wk), dexamethasone 4 mg PO BID Days 0, 1, 2 of each cycle for rash prophylaxis. Renal function is the dominant gating factor — avoid in CrCl <45. Counsel patients to hold OTC NSAIDs / aspirin around each cycle in renal insufficiency. Monitor CBC weekly through nadir, CMP each cycle, CT chest at any new respiratory symptom (ILD suspicion). UA: generic available; НСЗУ-reimbursed for indicated uses.
Де використовується
Regimens
REG-AMIVANTAMAB-CHEMO- Amivantamab + Carboplatin + Pemetrexed (NSCLC EGFR-mut post-osimertinib, MARIPOSA-2)REG-CARBO-PEM-MOD-ELDERLY- Carboplatin + Pemetrexed (attenuated, NSCLC non-squamous elderly ≥75y)REG-OSI-PEM-PLATINUM-NSCLC- Osimertinib + pemetrexed + carboplatin/cisplatin (FLAURA-2 regimen, EGFR-mut NSCLC, 1L)REG-PEMBRO-CHEMO-NEOADJ-NSCLC- Pembrolizumab + cisplatin-based chemo (NSCLC neoadjuvant; KEYNOTE-671)REG-PEMBRO-CHEMO-NSCLC-NONSQ- Pembrolizumab + carboplatin + pemetrexed (NSCLC non-squamous, 1L)REG-PEMETREXED-CISPLATIN-MPM- Pemetrexed + cisplatin (malignant pleural mesothelioma, 1L)