Pharmacokinetics of a granisetron transdermal system for the treatment of chemotherapy-induced nausea and vomiting

J Oncol Pharm Pract. 2009 Dec;15(4):223-31. doi: 10.1177/1078155209104063.


Objective: To determine the pharmacokinetic (PK) profile of granisetron transdermal formulation and examine its possible relationship with age, gender, and renal function.

Methods: This article describes a Phase I PK study and a post hoc pooled population PK analysis. The Phase I study was a randomized, cross-over study that assessed PK parameters of three granisetron patch sizes and oral granisetron. The pooled population PK analysis included data from three trials in healthy subjects (n = 48) and from Phase II and III studies in patients with cancer (n = 793). The population PK model was used to investigate granisetron exposure and its possible relationship with age, gender, and renal function.

Results: Following oral dosing, plasma granisetron concentration was quantifiable at 1 h, and maximal mean concentration (4.7 ng/mL) was reached 2 h after administration. With transdermal application, maximal concentration was reached 48 h post-application; t(1/2) was 36 h. With oral dosing, overall exposure after 5 days was 306 ng/mL.h, and C(avg) 2.6 ng/mL. This corresponded to an AUC(0-infinity) for the 52 cm(2) patch of 420 ng/mL.h and C(avg) 2.2 ng/mL over 6 days. Clearance was not affected by age, gender, weight, or renal function.

Conclusion: The 52 cm( 2) granisetron patch achieves a similar exposure to that of a 2 mg oral dose and provides continuous delivery of granisetron over 6 days. The patch may have utility in treating chemotherapy-induced nausea and vomiting where prolonged drug delivery is advantageous. No dose adjustments would be needed based on age or renal function.

Publication types

  • Clinical Trial, Phase I
  • Randomized Controlled Trial
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Administration, Cutaneous
  • Adolescent
  • Adult
  • Aging / metabolism
  • Antiemetics / administration & dosage
  • Antiemetics / pharmacokinetics*
  • Antiemetics / therapeutic use*
  • Antineoplastic Agents / adverse effects*
  • Area Under Curve
  • Biological Availability
  • Chemistry, Pharmaceutical
  • Creatinine / metabolism
  • Cross-Over Studies
  • Double-Blind Method
  • Female
  • Granisetron / administration & dosage
  • Granisetron / pharmacokinetics*
  • Granisetron / therapeutic use*
  • Half-Life
  • Humans
  • Male
  • Middle Aged
  • Nausea / chemically induced
  • Nausea / prevention & control*
  • Sex Characteristics
  • Vomiting / chemically induced
  • Vomiting / prevention & control*
  • Young Adult


  • Antiemetics
  • Antineoplastic Agents
  • Creatinine
  • Granisetron