CONJUGATE MONOMETHYL AURISTATIN E TO OBTAIN A COMPOSITION FOR TREATMENT OF PROSTATE CANCER

Provided is a conjugate of the formula (I) for treatment of tumors expressing PSMA, which comprises a PSMA-ligand with a linker and an antineoplastic agent monomethyl aluistatin E (MMAE). A composition for lyophilizate preparation based on the conjugate, a dosage form for therapy and obtained by the...

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Main Authors KHAZANOVA, Elena Sergeevna, RYBALOV, Aleksei Alekseevich, SKVORTSOV, Dmitrii Aleksandrovich, BER, Anton Petrovich, USPENSKAIA, Anastasiia Alekseevna, PCHELINTSEV, Svetozar Olegovich, GORELKIN, Petr Vladimitrovich, MAZHUGA, Aleksandr Georgievich, BELOGLAZKINA, Elena Kimovna, ZYK, Nikolai Petrovich, PETROV, Stanislav Aleksandrovich, MACHULKIN, Aleksei Ehduardovich, EROFEEV, Aleksandr Sergeevich, IVANENKOV, Ian Andreevich
Format Patent
LanguageEnglish
Published 08.09.2022
Subjects
CHEMISTRY
HETEROCYCLIC COMPOUNDS
HUMAN NECESSITIES
HYGIENE
MEDICAL OR VETERINARY SCIENCE
METALLURGY
ORGANIC CHEMISTRY
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
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Summary:Provided is a conjugate of the formula (I) for treatment of tumors expressing PSMA, which comprises a PSMA-ligand with a linker and an antineoplastic agent monomethyl aluistatin E (MMAE). A composition for lyophilizate preparation based on the conjugate, a dosage form for therapy and obtained by the lyophilization of the composition, PSMA expressing a prostate tumor growth inhibition, a solution for infusions or injections containing the dosage form, reconstituted by a solvent, comprising 95% ethyl alcohol and polysorbate 80 at a mass ratio (30-60 wt %):(70-40 wt %), respectively, also provided. It is possible to obtain high affinity and selectivity of the action of the conjugates in relation to PSMA expressing cells using the conjugate of the formula (I).
Bibliography:Application Number: US202217749958