• Pemetrexed inhibits dihydrofolate reductase, thymidylate synthase and glycinamide ribonucleotide formyltransferase with Ki values of 7 nM, 109 nM and 9.3 µM, respectively. Shih, C., et al. \"LY231514, a pyrrolo[2,3-d]pyrimidine-based antifolate that inhibits multiple folate-requiring enzymes.\" Cancer Res. 57: 1116-1123 (1997).
• Pemetrexed inhibits the proliferation of various human tumor cell lines, including CCRF-CEM leukemia, GC3/C1 colon carcinoma, and HCT-8 ileocecal carcinoma cells. Thymidine demonstrated its greatest protective effect at the IC50 of pemetrexed. However, higher drug concentrations of pemetrexed required the combination of both thymidine plus hypoxanthine to protect the tumor cells. Shih, C., et al. \"LY231514, a pyrrolo[2,3-d]pyrimidine-based antifolate that inhibits multiple folate-requiring enzymes.\" Cancer Res. 57: 1116-1123 (1997).
• The addition of folic acid supplementation with some antifolates substantially diminished the host toxicity. However, natural folates inhibited the activity of pemetrexed by suppressing folylpolyglutamate synthetase and thus decreasing the levels of active folylpolyglutamate pemetrexed congeners. Zhao, R., et al. \"Marked suppression of the activity of some, but not all, antifolate compounds by augmentation of folate cofactor pools within tumor cells.\" Biochem. Pharmacol. 61: 857-865 (2001).
• The membrane transport system for pemetrexed includes reduced folate carrier (RFC), folate receptors, a folate transport carrier with a low-pH optimum, and RFC-independent transport at neutral pH, etc. Chattopadhyay, S., et al. \"Pemetrexed: biochemical and cellular pharmacology, mechanisms, and clinical applications.\" Mol. Cancer Ther. 6: 404-417 (2007).
• Pemetrexed was approved in combination with cisplatin for the treatment of pleural mesothelioma in 2004. Hazarika, M., et al. \"FDA drug approval summaries: pemetrexed (Alimta®).\" Oncologist 9: 482-488 (2004).
• Pemetrexed was also approved for the second-line treatment of locally advanced or metastatic non-small cell lung cancer in 2004. Cohen, M.H., et al. \"FDA drug approval summary: pemetrexed for injection (Alimta®) for the treatment of non-small cell lung cancer.\" Oncologist 10: 363-368 (2005).
• Pemetrexed is the active ingredient in the drug sold under the trade name Alimta®. This drug has been approved in at least one country for use in patients with pleural mesothelioma as well as non-small cell lung cancer. NOTE: The pemetrexed product sold by LC Laboratories is NOT Alimta® and is NOT for human use.
• Our pemetrexed product is the disodium salt heptahydrate, whose CAS number is given above. The following CAS numbers correspond to other forms of pemetrexed: 137281-23-3 for the free acid; 150399-23-8 for the anhydrous disodium salt, and 357166-30-4 for the disodium salt \"hemipentahydrate\" (2.5 H2O).
• NOTE: Water content may vary from lot to lot. Please refer to the elemental analysis provided in the Certificate of Analysis to obtain the water content for each lot.
• Sold for laboratory or manufacturing purposes only; not for human, medical, veterinary, food, or household use.
• This product is offered for R&D use in accordance with (i) 35 USC 271(e)+A13(1) in the U.S.; (ii) Section 69.1 of Japanese Patent Law in Japan; (iii) Section 11, No. 2 of the German Patent Act of 1981 in Germany; (iv) Section 60, Paragraph 5b of the U.K. Patents Act of 1977 in the U.K.; (v) Sections 55.2(1) and 55.2(6) and other common law exemptions of Canadian patent law; (vi) Section 68B of the Patents Act of 1953 in New Zealand together with the amendment of same by the Statutes Amendment Bill of 2002; (vii) such related legislation and/or case law as may be or become applicable in the aforementioned countries; and (viii) such similar laws and rules as may apply in various other countries.
• Not available in some countries; not available to some institutions; not available for some uses.

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