Pemetrexed

(S) -2 - [4 - [2 - (4- amino-2- oxo-3 ,5,7- triazabicyclo [4.3.0 ] nona -3 ,8,10 -triene- 9-yl) - ethyl ] benzoyl] aminopentandicarbonsäure

  • C20H21N5O6 ( pemetrexed )
  • C20H19N5Na2O6 ( pemetrexed disodium · )

L01BA04

  • Folic acid analogs
  • Folic acid antagonist
  • Multi-target enzyme inhibitor
  • Cytostatics

Inhibition of enzymes

  • Thymidylate synthase (TS)
  • Dihydrofolate reductase (DHFR)
  • Glycinamide ribonucleotide formyl transferase ( GARFT ).
  • 427.41 g · mol -1 ( pemetrexed )
  • 471.37 g · mol -1 ( pemetrexed disodium · )

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Pemetrexed (brand name: Alimta ®, manufactured by Lilly ) is a drug that as a cytostatic agent ( antimetabolite ) is employed.

Mechanism of Action

As an analogue of folic acid, the active substance reaches at multiple sites into the DNA and RNA nucleotide synthesis and exerts its effect through the inhibition of the enzymes:

  • Thymidylate synthase (TS)
  • Dihydrofolate reductase (DHFR)
  • Glycinamide ribonucleotide formyl transferase ( GARFT ).

Indications

Pemetrexed is used both as monotherapy and in combination with cisplatin in numerous indications. As monotherapy ( NSCLC) is the treatment of locally advanced or metastatic non- small cell lung cancer used ( second-line therapy). The combination therapy with cisplatin is the treatment of advanced non- small cell lung cancer (NSCLC ) ( first line ) and malignant pleural mesothelioma of inoperable (MPM ) ( first-line ) in question.

Side effects

Side effects include ( selection) blood disorders, fever, hair loss, skin redness and rippling as well as nausea and vomiting.

Contraindications

Contraindications simultaneous vaccination against yellow fever as well as pregnancy and lactation apply.

CAS registry number PubChem Anatomical Therapeutic Chemical Classification System DrugBank Active ingredient
640791
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