Dr. Reddy's Laboratories, Incorporated

Ramesh Mullangi

Sriram K Rajagopal

Venkateswarlu Akella

Shanavas Alikunju

Subrahmanyam Duvvuri

Ajaya Kumar Reka

Raju Sirisilla

A 5(S)-(2'-hydroxyethoxy)-20(S)-camptothecin diasterisomer is described which is a better inhibitor of topoisomerase I than either the diastereoisomeric mixture 5(RS)-(2&#x2032;-hydroxyethoxy)-20(S)-camptothecin, or the 5(R)-(2&#x2032;-hydroxyethoxy)-20(S)-camptothecin diastereoisomer. Pharmaceutical compositions of the 5(S)-(2&#x2032;-hydroxyethoxy)-20(S)-camptothecin diastereoisomer are also described as are methods of using the compound for the inhibition of topoisomerase I and for the treatment of cancer.

5(S)-(2'-hydroxyethoxy)-20(S)-camptothecin and its preparation and use for the treatment of cancer

A crystalline form of 5(S)-(2'-hydroxyethoxy)-20(S)-camptothecin diastereoisomer of 5(RS)-(2&#x2032;-hydroxyethoxy)-20(S)-camptothecin is described that is characterized by having an X-ray powder diffraction pattern comprising one or more peak intensities expressed in degrees 2&#x3b8; that are selected from the group consisting of 7.2&#xb1;0.1, 9.4&#xb1;0.1, 11.02&#xb1;0.1, 12.00&#xb1;0.1, 14.54&#xb1;0.1, 15.2&#xb1;0.1, 18.92&#xb1;0.1, 21.86&#xb1;0.1, 22.74&#xb1;0.1 and 26.42&#xb1;0.1. Methods of making and using the compound are also described.

Crystalline form of 5(S)-(2-hydroxyethoxy)-20(S)-camptothecin

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Hyderabad Telangana, India

Ramesh Mullangi