Generic immunosuppressants

Pediatr Nephrol. 2018 Jul;33(7):1123-1131. doi: 10.1007/s00467-017-3735-z. Epub 2017 Jul 21.

Abstract

Immunosuppressive drugs for solid organ transplantation are critical dose drugs with a narrow therapeutic index. Many of the most commonly used innovator drugs are off patent and have been replicated by generic counterparts, often at substantial cost-savings to the patient. However, serious adverse events caused by the transition from innovator to generic medications, specifically in pediatric solid organ transplant recipients, have questioned these autosubstitutions. The purpose of this review is to summarize the criteria set forth by the regulatory bodies, and to examine how major immunosuppressive drugs conform to these recommendations. Regulatory bodies have established inconsistent criteria to demonstrate bioequivalence between innovator and generic medications, causing approved generic variations to have varying levels of equivalence with the innovator drugs. In order to minimize the risk for under-immunosuppression, the following recommendations have been concluded. Brand prescribing of cyclosporine and tacrolimus are recommended due to evidence of adverse events after conversion to generic formulations and differences in dissolution parameters. Mycophenolate mofetil (MMF) shows better bioequivalence between innovator and generic formulations, however caution should be advised when switching between formulations. The institution of 'innovator only' policies may be appropriate at this time in order to minimize the risk of under-immunosuppressing patients until the evidence of more stringent bioequivalence has been established.

Keywords: Antimetabolites; Calcineurin inhibitors; MMF; Sirolimus; Tacrolimus; mTOR inhibitors.

Publication types

  • Review

MeSH terms

  • Cyclosporine / pharmacokinetics
  • Cyclosporine / standards
  • Cyclosporine / therapeutic use
  • Drug Substitution / standards
  • Drugs, Generic / pharmacokinetics
  • Drugs, Generic / standards
  • Drugs, Generic / therapeutic use*
  • Graft Rejection / immunology
  • Graft Rejection / prevention & control*
  • Humans
  • Immunosuppression Therapy / methods*
  • Immunosuppression Therapy / standards
  • Immunosuppressive Agents / pharmacokinetics
  • Immunosuppressive Agents / standards
  • Immunosuppressive Agents / therapeutic use*
  • Mycophenolic Acid / pharmacokinetics
  • Mycophenolic Acid / standards
  • Mycophenolic Acid / therapeutic use
  • Organ Transplantation / adverse effects*
  • Randomized Controlled Trials as Topic
  • Tacrolimus / pharmacokinetics
  • Tacrolimus / standards
  • Tacrolimus / therapeutic use
  • Therapeutic Equivalency
  • Treatment Outcome
  • United States
  • United States Food and Drug Administration / standards

Substances

  • Drugs, Generic
  • Immunosuppressive Agents
  • Cyclosporine
  • Mycophenolic Acid
  • Tacrolimus