Drug intelligence / Profile preview

AMG 595

Development stage
Phase 1
Lead developer
Amgen
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules, Cytotoxic ADCs → Antibody-Drug Conjugates (ADCs) → Antibody Conjugates → Antibody-Based Therapeutics, Monoclonal Antibodies → Antibody-Based Therapeutics
Administration
Intravenous
01

Overview

AMG 595 is an investigational antibody-drug conjugate (ADC) developed for the treatment of glioblastoma multiforme (GBM) and other EGFRvIII-positive tumors. It consists of a human monoclonal antibody highly selective for the deletion-mutant epidermal growth factor receptor variant III (EGFRvIII), which is present in a subset of GBM patients, conjugated via a non-cleavable linker to the cytotoxic agent maytansinoid DM1. The mechanism of action involves specific binding to EGFRvIII-expressing tumor cells, internalization into the endo-lysosomal pathway, and subsequent release of DM1, which inhibits tubulin polymerization leading to mitotic arrest and apoptosis in targeted cancer cells. AMG 595 was developed by Amgen (originally Abgenix). Clinical development focused on recurrent glioblastoma multiforme and anaplastic astrocytoma[1][2][3][4][5][6].

Other names
anti-EGFRvIII antibody-drug conjugateanti-EGFRvIII-DM1 immunoconjugateanti-EGFRvIII-DM-1 immunoconjugateanti-EGFRvIII-DM 1 immunoconjugate
02

Targets

EGFRvIII (Epidermal growth factor receptor variant III)TUBB (Tubulin (alpha and beta subunits))

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