Drug intelligence / Profile preview

Lupartumab amadotin

Development stage
Discontinued
Lead developer
Bayer HealthCare Pharmaceuticals
Modality
Small Molecules, Cytotoxic ADCs → Antibody-Drug Conjugates (ADCs) → Antibody Conjugates → Antibody-Based Therapeutics, Monoclonal Antibodies → Antibody-Based Therapeutics
Administration
Intravenous
01

Overview

Lupartumab amadotin is an investigational antibody-drug conjugate (ADC) developed for the treatment of solid tumors that express the C4.4a antigen, also known as LYPD3 or LY6-PLAUR domain containing 3[1][2][3]. The drug consists of a monoclonal antibody targeting LYPD3 linked to a cytotoxic payload from the auristatin class (an anti-mitotic agent), designed to selectively deliver chemotherapy to tumor cells expressing this protein[2][3]. Its mechanism involves binding to LYPD3 on tumor cells, internalization of the ADC-antigen complex, and subsequent release of the cytotoxic agent inside the cell leading to cell death[8]. Developed by Bayer HealthCare, lupartumab amadotin reached phase 1 clinical trials for advanced malignant solid neoplasms but development has since been discontinued with no further active trials reported[2][5][6].

Other names
Anti-C4.4a antibody-drug conjugateAnti-C-4.4a antibody-drug conjugateAnti-C 4.4a antibody-drug conjugateAnti-LY6-PLAUR domain containing 3 antibody-drug conjugateAnti-LY-6-PLAUR domain containing 3 antibody-drug conjugateAnti-LY 6-PLAUR domain containing 3 antibody-drug conjugateAnti-LYPD3 antibody-drug conjugateAnti-LYPD-3 antibody-drug conjugateAnti-LYPD 3 antibody-drug conjugate
02

Targets

LYPD3TUBB (Tubulin (alpha and beta subunits))

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