Halofuginone

DB04866InvestigationalVet approvedSmall molecule

Halofuginone is a low molecular weight quinazolinone alkaloid, and a potent inhibitor of collagen alpha1(I) and matrix metalloproteinase 2 (MMP-2) gene expression. Halofuginone also effectively suppresses tumor progression and metastasis... Collgard Biopharmaceuticals is developing halofuginone for the treatment of scleroderma and received orphan drug designation from the U.S.

Mechanism: Halofuginone is a potent inhibitor of collagen a1(I) and matrix metalloproteinase 2 (MMP-2) gene expression. Halofuginone also suppresses extracellular matrix deposition and cell proliferation. The profound antitumoral effect of halofuginone is attributed to its combined inhibition of the tumor stromal support, vascularization, invasiveness, and cell proliferation.
Curator reviewed
Primary indication: For the treatment of scleroderma, cancer, and restenosis.Curator reviewed
Formula / weight: C₁₆H₁₇BrClN₃O₃ · 414.681 g/mol (avg)
Code names: HT-100

Resolves to

Compound

UNIIH84E4Y7HC9CAS55837-20-2ChEMBLCHEMBL1199540PubChem456390KEGGD04413

Structure

InChIKeyLVASCWIMLIKXLA-CABCVRRESA-NSMILES[H][C@]1(O)CCCN[C@]1([H])CC(=O)CN1C=NC2=C(C=C(Cl)C(Br)=C2)C1=O

Targets

P07814EPRS1P02452COL1A1P08253MMP2

What you can answer from here — as of August 30, 2026

3Protein targetsEach mapped to UniProt, with action and pharmacological action

Listed above

48Drug interactionsStructured to mechanism, not free text

4Clinical trialsPhase, status and sponsor resolved per trial

6+ReferencesStructured and connected to the statements they support

Which drugs share a target with Halofuginone, and which of those have an active Phase 3 trial?

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