Compositions and methods for oral delivery of crystalline triapine

Abstract

The present disclosure addresses this need by providing crystalline fine particle forms of 3-AP, methods for preparation and the treatment for solid tumors and hematological malignancies. In certain aspects, the present disclosure provides novel methods of preparing the compound of Formula I thereof, or 3-APs, crystalline fine particle forms of 3-AP, and compositions comprising them. In certain aspects, the present disclosure provides novel crystalline fine particle form of 3-AP which may provide advantages including improved bioavailability and stability relative to other crystalline or amorphous forms. In other aspects, the present disclosure provides oral dosage forms of crystalline fine particle form of 3-AP and excipients with improved stability. In additional aspects, the present disclosure provides novel methods of synthesizing novel crystalline fine particle form of 3-AP, preparing crystalline 3-AP particle delivery systems (PDS), and preparing novel final dosage forms (FDF) of crystalline fine particle 3-AP. In certain aspects, the present disclosure provides novel crystalline forms of fine particle 3-AP which may provide advantages including improved bioavailability and stability relative to other crystalline or amorphous forms.