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D3S-002
- Development stage
- Phase 2
- Lead developer
- D3 Bio
- Modality
- Bivalent/Multivalent Binders → Multivalent & Scaffold-Based Small Molecules → Small Molecules, Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules, Reversible Covalent Inhibitors → Covalent Small Molecules → Small Molecules, Allosteric Modulators → Classical Binding Small Molecules → Small Molecules, Irreversible Covalent Inhibitors → Covalent Small Molecules → Small Molecules, Fragment-Derived Small Molecules → Multivalent & Scaffold-Based Small Molecules → Small Molecules
- Administration
- Oral
01
Overview
D3S-002 is a novel, orally administered small molecule inhibitor targeting ERK1 and ERK2 kinases (extracellular-signal-regulated kinase 1/2). It is being developed for the treatment of advanced solid tumors, particularly those with mutations in the MAPK pathway. Preclinical studies have shown that D3S-002 demonstrates promising activity, selectivity, and a favorable safety profile. The drug has received FDA IND clearance and orphan drug designation, with first-in-human clinical trials currently underway to assess its safety, tolerability, pharmacokinetics, and recommended phase 2 dose in adults with advanced malignant solid neoplasms or MAPK mutation-positive solid tumors.
02
Targets
MAPK3 (Mitogen-activated protein kinase 1)
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