Alimta® (Pemetrexed)

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Pemetrexed: Pharmacokinetics

In PK studies, absorption of pemetrexed increased proportionally with dose increases. Pemetrexed has a volume of distribution of 16.1 L. Half-life is 3.5 hours. Pemetrexed has limited hepatic metabolism. Elimination occurs primarily in the urine.


Pharmacokinetic Properties

The information contained in this letter may not completely match the current local labeling for PEMETREXED. Please see local labeling approved in your country. 


  • Pemetrexed is for IV administration only.1
  • The PK of pemetrexed when administered as a single agent in doses ranging from 0.2 to 838 mg/m2 infused over a 10-minute period have been evaluated in 426 cancer patients with a variety of solid tumors. Pemetrexed total systemic exposure (AUC) and maximum plasma concentration (Cmax) increased proportionally with increase of dose. The PK of pemetrexed did not change over multiple treatment cycles.1


  • Pemetrexed has a steady-state volume of distribution of 16.1 liters. In vitro studies indicate that pemetrexed is approximately 81% bound to plasma proteins. Binding is not affected by degree of renal impairment.1


  • The total systemic clearance of pemetrexed is 91.8 mL/min and the elimination half-life of pemetrexed is 3.5 hours in patients with normal renal function (CrCl of 90 mL/min). As renal function decreases, the clearance of pemetrexed decreases and exposure (AUC) of pemetrexed increases.1


  • Pemetrexed is not metabolized to an appreciable extent.1


  • Pemetrexed is primarily eliminated in the urine, with 70% to 90% of the dose recovered unchanged within the first 24 hours following administration. In vitro studies indicated that pemetrexed is a substrate of OAT3, a transporter that is involved in the active secretion of pemetrexed.1

Additional PK Data

Information on the PK of pemetrexed in special populations and the effect of other medications on the PK of pemetrexed is available in the full prescribing information for pemetrexed.1


1Data on file, Eli Lilly and Company and/or one of its subsidiaries.


AUC = area under the curve

Cmax = maximum concentration

CrCl = creatinine clearance

IV = intravenous

OAT = organic anion transporter

PK = pharmacokinetic(s)

Fecha de la última revisión: 2019 M10 14

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