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Laprituximab emtansine (IMGN-289) is an immunotoxin targeting HER1. Laprituximab emtansine is an EGFR antibody-drug conjugate (ADC) consisting of the J2898A antibody, DM1 (anti-microtubule agent) and the SMCC thioether linker. Laprituximab emtansine can be used for cancer research[1][2][3]. | [in vivo]
Laprituximab emtansine (1-5 mg/kg, i.v.) results tumor regression in EGFR-positive SCCHN xenograft model[4].
| Animal Model: | EGFR-positive SCCHN xenograft model[4] | | Dosage: | 1, 2.5, 5 mg/kg | | Administration: | i.v. | | Result: | Resulted tumor regression with a minimally efficacious dose of 1 mg/kg, and highly active at 2.5 and 5 mg/kg. |
| [IC 50]
HER1 | [References]
[1] Moradi-Kalbolandi S, et al. Monoclonal antibody-based therapeutics, targeting the epidermal growth factor receptor family: from herceptin to Pan HER. J Pharm Pharmacol. 2018 Jul;70(7):841-854. DOI:10.1111/jphp.12911
[2] Yulius Y. et al. Abstract 4513: IMGN289, an EGFR-targeting antibody-drug conjugate, is effective against tumor cells that are resistant to EGFR tyrosine kinase inhibitors. Cancer Res 1 October 2014; 74 (19_Supplement): 4513.
[3] Hyunseok Kang, et al. Antitumor effect of IMGN289, an anti-EGFR antibody-drug conjugate (ADC), in preclinical models of head and neck squamous cell carcinomas (HNSCC). Journal of Clinical Oncology. 2014. 32, no. 15_suppl.
[4] Jose F. Ponte, et al. Abstract 5483: Preclinical evaluation of IMGN289, an anti-EGFR antibody-maytansinoid conjugate for the treatment of squamous cell carcinoma of the head and neck. Cancer Res (2013) 73 (8_Supplement): 5483. |
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