Erlotinib

From Anvita Health Wiki

Contents 1 Introduction 2 Indications 3 Dosage 4 Pharmacokinetics 5 Adverse-effects 6 Drug-interactions 7 Mechanism-of-action 8 Notes 9 More General Terms 10 Internet Database 11 References

Introduction

• Tradename: Tarceva

Indications

• non-small-cell lung carcinoma,

• alternative to docetaxel
• second-line treatment option [6] { NGC, }
• extends life 2 months longer than placebo [1,2]

• pancreatic cancer, adjunct to gemcitabine

Dosage

• 100-150 mg PO QD

Pharmacokinetics

• metabolized by cyt P450 3A4

Adverse-effects

• diarrhea
• rash
• increased liver function tests
• interstitial lung disease (small risk)

• cough, fever, dyspnea

• cases of hepatic failure & hepatorenal syndrome, including fatalities [4]
• gastrointestinal perforation (including fatalities) [5]
• bullous, blistering and exfoliative skin conditions: [5]

• Stevens-Johnson syndrome
• toxic epidermal necrolysis
• in some cases fatal

• corneal perforation, corneal ulceration [5]

Drug-interactions

• drugs that induce of inhibit cyt P450 3A4

Mechanism-of-action

• inhibits tyrosine kinase activity of EGF receptor

Notes

• Cost = $2000/month

More General Terms

• antineoplastic agent (chemotherapeutic agent)

Internet Database

PubChem: 176870
PubChem: 176871

References

1. Prescriber's Letter 12(1):5 2005 FDA Approves New Drug for the Most Common Type of Lung Cancer Detail-Document#: [1] (subscription needed) [2]
2. Journal Watch 25(17):136, 2005 Shepherd FA, Rodrigues Pereira J, Ciuleanu T, Tan EH, Hirsh V, Thongprasert S, Campos D, Maoleekoonpiroj S, Smylie M, Martins R, van Kooten M, Dediu M, Findlay B, Tu D, Johnston D, Bezjak A, Clark G, Santabarbara P, Seymour L; National Cancer Institute of Canada Clinical Trials Group. Erlotinib in previously treated non-small-cell lung cancer. N Engl J Med. 2005 Jul 14;353(2):123-32. PMID: [3]
   - Tsao MS, Sakurada A, Cutz JC, Zhu CQ, Kamel-Reid S, Squire J, Lorimer I, Zhang T, Liu N, Daneshmand M, Marrano P, da Cunha Santos G, Lagarde A, Richardson F, Seymour L, Whitehead M, Ding K, Pater J, Shepherd FA. Erlotinib in lung cancer - molecular and clinical predictors of outcome. N Engl J Med. 2005 Jul 14;353(2):133-44. PMID: [4]
   - Doroshow JH. Targeting EGFR in non-small-cell lung cancer. N Engl J Med. 2005 Jul 14;353(2):200-2. No abstract available. PMID: [5]
3. Moore MJ, Goldstein D, Hamm J, Figer A, Hecht JR, Gallinger S, Au HJ, Murawa P, Walde D, Wolff RA, Campos D, Lim R, Ding K, Clark G, Voskoglou-Nomikos T, Ptasynski M, Erlotinib Plus Gemcitabine Compared With Gemcitabine Alone in Patients With Advanced Pancreatic Cancer: A Phase III Trial of the National Cancer Institute of Canada Clinical Trials Group. J Clin Oncol. 2007 Apr 23; [Epub ahead of print] PMID: [6]
4. FDA MedWatch [7]
5. FDA MedWatch [8]
6. National Guideline Clearinghouse Erlotinib for the treatment of non-small-cell lung cancer. National Institute for Health and Clinical Excellence ngc-guideline: [9]

erlotinib (Tarceva)