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1. (WO2018200462) DRUG CONJUGATES WITH PHOTOCLEAVABLE SOLUBILITY MODULATORS

Pub. No.:    WO/2018/200462    International Application No.:    PCT/US2018/029056
Publication Date: Fri Nov 02 00:59:59 CET 2018 International Filing Date: Wed Apr 25 01:59:59 CEST 2018
IPC: A61K 38/28
A61K 41/00
A61N 5/06
C08F 8/32
C08G 73/02
Applicants: FRIEDMAN, Simon, H.
NADENDLA, Karthik
SARODE, Bhagyesh
JAIN, Piyush
KARUNAKARAN, Dipu
CHINTALA, Swetha
SHAH, Parth
Inventors: FRIEDMAN, Simon, H.
NADENDLA, Karthik
SARODE, Bhagyesh
JAIN, Piyush
KARUNAKARAN, Dipu
CHINTALA, Swetha
SHAH, Parth
Title: DRUG CONJUGATES WITH PHOTOCLEAVABLE SOLUBILITY MODULATORS
Abstract:
The present invention is directed to a composition suitable for forming an implanted light activated drug depot, methods of making the composition, and methods and systems for using the composition. The composition comprises a plurality of drug conjugates, which comprise a drug molecule and a small solubility modulating portion. The drug conjugates are insoluble upon implantation as a drug depot into a subject, and the drug is preferably soluble once cleaved from the depot. One aspect of the invention is directed to a drug conjugate having a modulating portion that modifies the solubility of the drug conjugate by employing a hydrophobic non-polar moiety. Another aspect of the invention is directed to a drug conjugate having a modulating portion that modifies the solubility of the drug by employing a charged moiety that shifts the isoelectric point of the drug conjugate to a physiological pH.