Drug intelligence / Profile preview

NN2101-DM1

Development stage
Preclinical
Lead developer
Novelty Nobility
Modality
Cytotoxic ADCs → Antibody-Drug Conjugates (ADCs) → Antibody Conjugates → Antibody-Based Therapeutics, Monoclonal Antibodies → Antibody-Based Therapeutics
Administration
Intravenous
01

Overview

NN2101-DM1 is a preclinical antibody-drug conjugate (ADC) developed by Novelty Nobility as a proof-of-concept molecule for targeting cKIT-positive malignancies. It consists of a fully human anti-cKIT monoclonal antibody (NN2101) conjugated to the microtubule-inhibitory payload DM1 (mertansine) via a non-cleavable SMCC linker. This linker-payload system is the same as that used in ado-trastuzumab emtansine. NN2101-DM1 demonstrated therapeutic efficacy in preclinical models of small cell lung cancer (SCLC) and gastrointestinal stromal tumors (GIST). However, due to inherent limitations such as heterogeneous drug-antibody ratios and potential resistance to SMCC-DM1 cleavage, the program was optimized into NN3201, which utilizes a site-specific cleavable linker and an MMAE payload.

02

Targets

TUBB (Tubulin (alpha and beta subunits))KIT (c-KIT proto-oncogene receptor tyrosine kinase)

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