Abstract: This invention relates to a solid phase method of synthesizing biomolecule-drug conjugates. In particular, this invention relates to a solid phase method of synthesizing antibody-drug conjugates (ADCs). This invention also relates to intermediate methods of producing immobilized, chemically modified biomolecules, e.g. antibodies. The invention also relates to various uses of capture resins and to biomolecule-drug conjugates, intermediate products and compositions prepared by the methods of the invention.
Abstract: The invention relates to a lock-release method to be applied to biomolecules, such as antibodies, to improve the purification, production, stability and storage of biomolecules. A biomolecule is covalently bound to a polymer support comprising a diketone group so that the biomolecule can be purified, produced and/or stored before being released from the support. The diketone group of the polymer support is a 1,3-ketoester, 1,3-ketothioester or 1,3-ketoamide is a group of Formula (1): R1 is an optionally substituted hydrocarbyl, perhalogenated hydrocarbyl, or a heterocyclyl group; Y is hydrogen, an optionally substituted hydrocarbyl, or a heterocyclyl group; X is —O, —NR2 or —S, wherein the free valence of —O, —NR2 or —S is bonded to the support optionally via a linker; and R2 is hydrogen, an optionally substituted hydrocarbyl, or a heterocyclyl group. The invention also relates to a polymer support comprising the diketone group.