Abstract
AbstractDrug–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...
Sign-in/Register to access full text options 
Talk to us
Join us for a 30 min session where you can share your feedback and ask us any queries you have
Schedule a callDisclaimer: All third-party content on this website/platform is and will remain the property of their respective owners and is provided on "as is" basis without any warranties, express or implied. Use of third-party content does not indicate any affiliation, sponsorship with or endorsement by them. Any references to third-party content is to identify the corresponding services and shall be considered fair use under The CopyrightLaw.
