Imatinib

From Anvita Health Wiki

Contents 1 Introduction 2 Indications 3 Dosage 4 Monitor 5 Adverse-effects 6 Mechanism-of-action 7 Notes 8 More General Terms 9 Internet Database 10 References

Introduction

• Tradename: Gleevec ( imatinib mesylate), formerly STI571

Indications

• chronic myeloid leukemia* ( CML) [2,3,4]

• * may be drug of choice for CML

Dosage

• given PO QD

Monitor

• complete blood count ( CBC)
• liver function tests ( serum AST, serum ALT serum alkaline phosphatase) baseline, monthly, & as clinically indicated [7]

Adverse-effects

• edema
• nausea
• muscle cramps
• neutropenia
• thrombocytopenia
• severe congestive heart failure [6]

• left ventricular dysfunction

• hepatotoxicity [7]

• * adverse effects severe enough to cause discontinuation of therapy in 2% of patients [2]

Mechanism-of-action

• binds to & blocks ABL1 & ABL2 that stimulates proliferation of abnormal leukocytes (including BCR-ABL)
• binds to different site than BMS-354825

Notes

• Manufacturer: Novartis

More General Terms

• antineoplastic agent (chemotherapeutic agent)
• protein kinase inhibitor

Internet Database

PubChem: 123596
PubChem: 5291

References

1. Prescriber's Letter 8(6):34 2001
2. Journal Watch 22(7):53, 2002 Kantarjian H et al, N Engl J Med 346:645, 2002 Savage DG & Antman KH, N Engl J Med 346:683, 2002
3. Journal Watch 21(9):72, 2001 Druker et al, N Engl J Med 344:1031, 2001 Druker et al, N Engl J Med 344:1038, 2001 Goldman & Melo, N Engl J Med 344:1084, 2001
4. Journal Watch 23(8):63-64, 2003 O'Brien SG et al, N Engl J Med 348:994, 2003 Pegg K & Mackinnon S, N Engl J Med 348:1048, 2003
5. Department of Veterans Affairs, VA National Formulary
   - restricted to hematology/oncology
6. FDA MedWatch [1]
7. Prescriber's Letter 17(7): 2010 Recommended Lab Monitoring for Common Medications Liver Function Test Scheduling Detail-Document#: [2] (subscription needed) [3]
8. National Guideline Clearinghouse Treatment of chronic myeloid leukemia with imatinib. Program in Evidence-based Care ngc-guideline: [4]
   - Imatinib for the treatment of unresectable and/or metastatic gastrointestinal stromal tumours. (National Institute for Health and Clinical Excellence) ngc-guideline: [5]
   - Imatinib mesylate in the adjuvant treatment of gastrointestinal stromal tumours (GIST). Program in Evidence-based Care ngc-guideline: [6]
   - Imatinib for the adjuvant treatment of gastrointestinal stromal tumours. National Institute for Health and Clinical Excellence (NICE) ngc-guideline: [7]

imatinib (Gleevec)