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torcetrapib

Indications: -> hypoalphalipoproteinemia Dosage: 10-120 mg PO BID Adverse effects: (reported in clinical trials) 1) dizziness 2) headache 3) asthenia 4) pain 5) dyspepsia 6) reactivation of Herpes simplex 7) shingles (Herpes zoster) 8) sweating 9) amnesia 10) abnormal thinking 11) increases cardiovascular events & all-cause mortality [6] Laboratory: - adverse effects on serum aldosterone & serum HCO3- Mechanism of action: 1) inhibition of cholesteryl ester transfer protein 2) increases HDL cholesterol by 16-91% (dose-dependent) [3] a) 61% for dose of 120 mg BID in combination with 20 mg of atorvastatin QD [1] b) despite increasing HDL, increases cardiovascular events & all-cause mortality [6] 3) reduces LDL cholesterol 17% in combination with atorvastatin

Interactions

drug adverse effects of anti-hyperlipidemic agents

General

cholesteryl ester transfer protein (CETP) inhibitor

Database Correlations

PUBCHEM cid=159325

References

  1. Brousseau ME, Schaefer EJ, Wolfe ML, Bloedon LT, Digenio AG, Clark RW, Mancuso JP, Rader DJ. Effects of an inhibitor of cholesteryl ester transfer protein on HDL cholesterol. N Engl J Med. 2004 Apr 8;350(15):1505-15. PMID: 15071125
  2. Brewer HB Jr. Increasing HDL Cholesterol Levels. N Engl J Med. 2004 Apr 8;350(15):1491-4. No abstract available. PMID: 15071124
  3. Clark RW, Sutfin TA, Ruggeri RB, Willauer AT, Sugarman ED, Magnus-Aryitey G, Cosgrove PG, Sand TM, Wester RT, Williams JA, Perlman ME, Bamberger MJ. Raising high-density lipoprotein in humans through inhibition of cholesteryl ester transfer protein: an initial multidose study of torcetrapib. Arterioscler Thromb Vasc Biol. 2004 Mar;24(3):490-7. Epub 2004 Jan 22. PMID: 14739125
  4. Bays H, Stein EA. Pharmacotherapy for dyslipidaemia--current therapies and future agents. Expert Opin Pharmacother. 2003 Nov;4(11):1901-38. Review. PMID: 14596646
  5. Prescriber's Letter 11(5):27 2004 Detail-Document#: 200504 (subscription needed) http://www.prescribersletter.com
  6. Barter PJ et al, Effects of torcetrapib in patients at high risk for coronary events. N Engl J Med 2007, 357:2109 PMID: 17984165