Aminopterin—Monoclonal antibody conjugates: antitumor activity and toxicity

Autor:	Geoffrey A. Pietersz, Ron Bell, Kenia G. Krauer
Rok vydání:	1993
Předmět:	Drug endocrine system biology medicine.drug_class Chemistry media_common.quotation_subject Pharmaceutical Science General Medicine Pharmacology Aminopterin Monoclonal antibody In vivo Toxicity medicine biology.protein Methotrexate Antibody medicine.drug Conjugate media_common
Zdroj:	Drug Delivery. 1:27-33
ISSN:	1521-0464 1071-7544
DOI:	10.3109/10717549309031338
Popis:	Drug–antibody conjugates are undergoing close scrutiny as new antitumor agents because they confer increased drug specificity, producing higher accumulation in the tumor and less systemic toxicity than free drug. Consequently this has led to the use of drugs more toxic than those that can normally be used. How-ever, contrary to these conclusions immunoconjugates containing aminopterin (AMN), while having potent antitumor activity, are more toxic than free drug. AMN, a more toxic analog of the folic acid antagonist methotrexate (MTX), was coupled to the anti-Ly-2.1 antibody and the in vivo activity of the conjugate was tested against the Ly-2.1+ murine thymoma ITT(1)75NS E3 (E3). The aminopterin conjugates had molar ratios of 4–6 residues of AMN per MoAb molecule and retained 50% of the original antibody activity. A single dose of 75 μg AMN-anti-Ly-2.1 inhibited tumor growth by 30% and injection of 105 μg AMN–MoAb conjugate, in three doses, caused 63% tumor growth inhibition. Considerably higher do...
Databáze:	OpenAIRE
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