imatinib (Gleevec)
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Introduction
Tradename: Gleevec (imatinib mesylate), formerly STI571
Indications
- chronic myeloid leukemia* (CML)[2][3][4][9]
- Philadelphia chromosome-positive ALL[10]
- chronic eosinophilic leukemia
- hypereosinophilic syndrome[10]
- lung cancer
- gastrointestinal stromal tumor
- pancreatic cancer[9]
- dermatofibrosarcoma protuberans[10]
- systemic mastocytosis[10]
- scleroderma ?[12]
* may be drug of choice for CML
Dosage
Monitor
- complete blood count (CBC)
- liver function tests (serum AST, serum ALT serum alkaline phosphatase) baseline, monthly, & as clinically indicated[7]
* also see ARUP consult []
Adverse effects
- edema
- nausea
- muscle cramps
- neutropenia
- thrombocytopenia
- severe congestive heart failure[6]
- hepatotoxicity[7]
- rash
- fatigue
- diarrhea[9]
* 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
- inhibits CSF1R
- inhibits EGFR[9]
- inhibits GSAP, thus may inhibit beta-amyloid production[11]
Notes
- Manufacturer: Novartis
- price tripled from $30,000 per year in the U.S. at its 2001 introduction to over $90,000 in 2012[8]
More general terms
References
- ↑ Prescriber's Letter 8(6):34 2001
- ↑ 2.0 2.1 2.2 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
- ↑ 3.0 3.1 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
- ↑ 4.0 4.1 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
- ↑ Department of Veterans Affairs, VA National Formulary
restricted to hematology/oncology - ↑ 6.0 6.1 FDA MedWatch http://www.fda.gov/medwatch/safety/2006/safety06.htm#Gleevec
- ↑ 7.0 7.1 7.2 Prescriber's Letter 17(7): 2010 Recommended Lab Monitoring for Common Medications Liver Function Test Scheduling Detail-Document#: http://prescribersletter.com/(5bhgn1a4ni4cyp2tvybwfh55)/pl/ArticleDD.aspx?li=1&st=1&cs=&s=PRL&pt=3&fpt=25&dd=260704&pb=PRL (subscription needed) http://www.prescribersletter.com
- ↑ 8.0 8.1 Experts in chronic myeloid leukemia Price of drugs for chronic myeloid leukemia (CML), reflection of the unsustainable cancer drug prices: perspective of CML experts. Blood. April 15, 2013 <PubMed> PMID: https://www.ncbi.nlm.nih.gov/pubmed/23620577 <Internet> http://bloodjournal.hematologylibrary.org/content/early/2013/04/23/blood-2013-03-490003.full.pdf+html
- ↑ 9.0 9.1 9.2 9.3 9.4 Medical Knowledge Self Assessment Program (MKSAP) 16, 18. American College of Physicians, Philadelphia 2012, 2018.
- ↑ 10.0 10.1 10.2 10.3 10.4 Deprecated Reference
- ↑ 11.0 11.1 He G, Luo W, Li P, Remmers C Gamma-secretase activating protein is a therapeutic target for Alzheimer's disease. Nature. 2010 Sep 2;467(7311):95-8 PMID: https://www.ncbi.nlm.nih.gov/pubmed/20811458
- ↑ 12.0 12.1 Spiera RF, Gordon JK, Mersten JN et al Imatinib mesylate (Gleevec) in the treatment of diffuse cutaneous systemic sclerosis: results of a 1-year, phase IIa, single-arm, open-label clinical trial. Ann Rheum Dis. 2011 Jun;70(6):1003-9. PMID: https://www.ncbi.nlm.nih.gov/pubmed/21398330
- ↑ ARUP Consult: Imatinib Therapeutic Drug Monitoring https://arupconsult.com/ati/imatinib-therapeutic-drug-monitoring