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Bioinformatics Database on
"Radiosensitisers and Radioprotectors"

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Effective dose
Mode and form of
oral and IV[2]
Time of
before irradiation[3],[4]
concurrent with irradiation[5],[6]
Side Effects: oral mucositis is often the limiting side effect of Methotrexate administration.[7]
Combined action
with other drugs
Co-administration of methotrexate, paclitaxel, or doxorubicin enhanced the cytotoxicity of 111In-NLS-trastuzumab toward human breast cancer 231-H2N and TrR1 cells n vitro.[5]
Toxicity was increased when Misonidazole or Metronidazole were combined with Methotrexate in C3H male mice.[8]
prior administration of Folic acid and post-treatment with Folinic acid reduces the germ cell toxicity induced by Methotrexate in mice.[9]
Precautions &
1. Kassis AI et al, Therapeutic potential of 5-[125I]iodo-2’-deoxyuridine and methotrexate in the treatment of advanced neoplastic meningitis. Int J Radiat Biol 2004;80(11–12): 941–946.
2. Lustig RA, DeMare PA, Kramer S, Adjuvant methotrexate in the radiotherapeutic management of advanced tumors of the head and neck. Cancer. 1976;37(6):2703-8.
3. Geyer JR et al, Radiation, methotrexate, and white matter necrosis: laboratory evidence for neural radioprotection with preirradiation methotrexate.Int J Radiat Oncol Biol Phys. 1988 ;15(2):373-5.
4. Morris AD, Hopewell JW, Combined effects of radiation and methotrexate on the cells of the rat subependymal plate. J R Soc Med. 1983 ;76(10):848-52.
5. Costantini DL et al, Methotrexate, Paclitaxel, and Doxorubicin radiosensitize HER2-Amplified human breast cancer cells to the Auger electron–emitting radiotherapeutic agent 111In-NLS-Trastuzumab. J Nucl Med 2010; 51:477–483.
6. Costantini DL et al, Trastuzumab-resistant breast cancer cells remain sensitive to the Auger electron–emitting radiotherapeutic agent 111In-NLS-Trastuzumab and are radiosensitized by Methotrexate. J Nucl Med 2008; 49:1498–1505.
7. Spittle MF, Methotrexate and radiation. Int J Radiat Oncol Biol Phys. 1978 ;4(1-2):103-7.
8. Tannock IF, In vivo interaction of anti-cancer drugs with misonidazole or metronidazole: methotrexate, 5-fluorouracil and adriamycin. Br J Cancer. 1980; 42(6): 861–870.
9. Padmanabhan S et al, Methotrexate-induced cytotoxicity and genotoxicity in germ cells of mice: Intervention of folic and folinic acid. Mutat Res 2009; 673(1): 43–52.