Selected Immunosuppressants; Temsirolimus/Protease Inhibitors; Cobicistat Interactions

This information is generalized and not intended as specific medical advice. Consult your healthcare professional before taking or discontinuing any drug or commencing any course of treatment.

Medical warning:

Serious. These medicines may interact and cause very harmful effects. Contact your healthcare professional (e.g. doctor or pharmacist) for more information.

How the interaction occurs:

Protease inhibitors and cobicistat may slow down how quickly your body processes cyclosporine, sirolimus, tacrolimus, or temsirolimus.

What might happen:

The amount of cyclosporine, sirolimus, tacrolimus, or temsirolimus in your body may increase and cause more side effects than normal.

What you should do about this interaction:

Make sure your healthcare professionals (e.g. doctor or pharmacist) know that you are taking these two medicines together. Your doctor may need to check the amount of cyclosporine, sirolimus, tacrolimus, or temsirolimus in your blood and adjust the dose until you have been stabilized on the combination.Contact your healthcare professional if you experience any chest discomfort, dizziness, shaking, leg cramping, swelling, or any unusual stomach upset, headache, or skin irritation.Your healthcare professionals may already be aware of this interaction and may be monitoring you for it. Do not start, stop, or change the dosage of any medicine before checking with them first.

  • 1.Sparkes T, Lemonovich TL. Interactions between anti-infective agents and immunosuppressants-Guidelines from the American Society of Transplantation Infectious Diseases Community of Practice. Clin Transplant 2019 Feb 28; e13510.
  • 2.Torisel (temsirolimus) US prescribing information. Wyeth Pharmaceuticals, Inc. March, 2018.
  • 3.Victrelis (boceprevir) US prescribing information. Schering Corporation January, 2017.
  • 4.Incivek (telaprevir) US prescribing information. Vertex Pharmaceuticals Incorporated October, 2013.
  • 5.Agenerase (amprenavir) Capsules US prescribing information. GlaxoSmithKline May, 2005.
  • 6.Reyataz (atazanavir sulfate) US prescribing information. Bristol-Myers Squibb Company September, 2020.
  • 7.Tybost (cobicistat) US prescribing information. Gilead Sciences, Inc. August, 2020.
  • 8.Prezista (darunavir) US prescribing information. Tibotec Inc. May, 2019.
  • 9.Lexiva (fosamprenavir calcium) US prescribing information. GlaxoSmithKline March, 2019.
  • 10.Crixivan (indinavir sulfate) US prescribing information. Merck & Co., Inc. September, 2016.
  • 11.Kaletra (lopinavir/ritonavir tablets) US prescribing information. Abbott Laboratories December, 2019.
  • 12.Viracept (nelfinavir mesylate) US prescribing information. Agouron Pharmaceuticals, Inc. September, 2016.
  • 13.Norvir (ritonavir) US prescribing information. Abbott Laboratories December, 2019.
  • 14.Invirase (saquinavir mesylate) US prescribing information. Roche Laboratories, Inc. March, 2019.
  • 15.Aptivus (tipranavir) US prescribing information. Boehringer Ingelheim Pharmaceuticals, Inc. June, 2020.
  • 16.Rollins B, Farouk S, DeBoccardo G, Lerner S, Rana M, Huprikar S, Miko L, Delaney V, Florman S, Shapiro R. Higher rates of rejection in HIV-infected kidney transplant recipients on ritonavir-boosted protease inhibitors: 3-year follow-up study. Clin Transplant 2019 Jun; 33(6):e13534.
  • 17.Guaraldi G, Cocchi S, Codeluppi M, Di Benedetto F, Bonora S, Motta A, Luzi K, Pecorari M, Gennari W, Masetti M, Gerunda GE, Esposito R. Pharmacokinetic interaction between Amprenavir/Ritonavir and FosAmprenavir on cyclosporine in two patients with human immunodeficiency virus infection undergoing orthotopic liver transplantation. Transplant Proc 2006 May;38(4):1138-40.
  • 18.Vogel M, Voigt E, Michaelis HC, Sudhop T, Wolff M, Turler A, Sauerbruch T, Rockstroh JK, Spengler U. Management of drug-to-drug interactions between cyclosporine A and the protease-inhibitor lopinavir/ritonavir in liver-transplanted HIV-infected patients. Liver Transpl 2004 Jul; 10(7):939-44.
  • 19.Frassetto L, Thai T, Aggarwal AM, Bucher P, Jacobsen W, Christians U, Benet LZ, Floren LC. Pharmacokinetic interactions between cyclosporine and protease inhibitors in HIV+ subjects. Drug Metab Pharmacokinet 2003; 18(2):114-20.
  • 20.Brinkman K, Huysmans F, Burger DM. Pharmacokinetic interaction between saquinavir and cyclosporine. Ann Intern Med 1998 Dec 1;129(11):914-5.
  • 21.Jain AK, Venkataramanan R, Fridell JA, Gadomski M, Shaw LM, Ragni M, Korecka M, Fung J. Nelfinavir, a protease inhibitor, increases sirolimus levels in a liver transplantation patient: a case report. Liver Transpl 2002 Sep;8(9):838-40.
  • 22.Han Z, Kane BM, Petty LA, Josephson MA, Sutor J, Pursell KJ. Cobicistat Significantly Increases Tacrolimus Serum Concentrations in a Renal Transplant Recipient with Human Immunodeficiency Virus Infection. Pharmacotherapy 2016 Jun;36(6):e50-e53.
  • 23.Mertz D, Battegay M, Marzolini C, Mayr M. Drug-drug interaction in a kidney transplant recipient receiving HIV salvage therapy and tacrolimus. Am J Kidney Dis 2009 Jul;54(1):e1-4.
  • 24.Jain AK, Venkataramanan R, Shapiro R, Scantlebury VP, Potdar S, Bonham CA, Ragni M, Fung JJ. The interaction between antiretroviral agents and tacrolimus in liver and kidney transplant patients. Liver Transpl 2002 Sep;8(9):841-5.
  • 25.Schonder KS, Shullo MA, Okusanya O. Tacrolimus and lopinavir/ritonavir interaction in liver transplantation. Ann Pharmacother 2003 Dec; 37(12):1793-6.
  • 26.Jain AB, Venkataramanan R, Eghtesad B, Marcos A, Ragni M, Shapiro R, Rafail AB, Fung JJ. Effect of coadministered lopinavir and ritonavir (Kaletra) on tacrolimus blood concentration in liver transplantation patients. Liver Transpl 2003 Sep;9(9):954-60.
  • 27.Guaraldi G, Cocchi S, Codeluppi M, Di Benedetto F, Bonora S, Pecorari M, Gennari W, Cautero N, Pinna AD, Gerunda GE, Esposito R. Role of therapeutic drug monitoring in a patient with human immunodeficiency virus infection and end-stage liver disease undergoing orthotopic liver transplantation. Transplant Proc 2005 Jul-Aug;37(6):2609-10.
  • 28.Schvarcz R, Rudbeck G, Soderdahl G, Stahle L. Interaction between nelfinavir and tacrolimus after orthoptic liver transplantation in a patient coinfected with HIV and hepatitis C virus (HCV). Transplantation 2000 May 27;69(10):2194-5.
  • 29.Sheikh AM, Wolf DC, Lebovics E, Goldberg R, Horowitz HW. Concomitant human immunodeficiency virus protease inhibitor therapy markedly reduces tacrolimus metabolism and increases blood levels. Transplantation 1999 Jul 27;68(2):307-9.

Selected from data included with permission and copyrighted by First Databank, Inc. This copyrighted material has been downloaded from a licensed data provider and is not for distribution, except as may be authorized by the applicable terms of use.

CONDITIONS OF USE: The information in this database is intended to supplement, not substitute for, the expertise and judgment of healthcare professionals. The information is not intended to cover all possible uses, directions, precautions, drug interactions or adverse effects, nor should it be construed to indicate that use of a particular drug is safe, appropriate or effective for you or anyone else. A healthcare professional should be consulted before taking any drug, changing any diet or commencing or discontinuing any course of treatment.