Description

Simple

Clinical

Overview

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 in mice. Collgard Biopharmaceuticals is developing halofuginone for the treatment of scleroderma and received orphan drug designation from the U.S. Food and Drug Administration in March, 2000.

Pharmacology

Indication

For the treatment of scleroderma, cancer, and restenosis.

Pharmacodynamic

Halofuginone, a fully synthetic small molecule, is a potent and selective regulator of stromal cell activation, cell migration and Collagen type I synthesis, a process that has been identified as a 'master switch' in the body's tissue repair process.

Mechanism of action

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 stro... Read more

Absorption

Readily bioavailable and rapidly absorbed following oral administration.

Protein binding

Information currently not available.

Volume of distribution

Information currently not available.

Clearance

Information currently not available.

Half life

23.8 to 72.1 hours

Route of elimination

Information currently not available.

Toxicity

Information currently not available.

Adverse Effects

Contraindications

Information currently not available.

Food Interactions

    Information currently not available.

Interactions

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  • Paracetamol(acetaminophen)
  • Paxil(paroxetine)
  • Pamelor(nortriptyline)
  • Panadol(acetaminophen)
  • Patanol(olopatadine ophthalmic)
  • Pataday(olopatadine ophthalmic)
  • Parnate(tranylcypromine)
  • Pazeo(olopatadine ophthalmic)
Alendronic acid
The risk or severity of jaw osteonecrosis and anti-angiogenesis can be increased when Halofuginone is combined with Alendronic acid.
Clodronic acid
The risk or severity of jaw osteonecrosis and anti-angiogenesis can be increased when Halofuginone is combined with Clodronic acid.
Darbepoetin alfa
The risk or severity of Thrombosis can be increased when Darbepoetin alfa is combined with Halofuginone.
Erythropoietin
The risk or severity of Thrombosis can be increased when Erythropoietin is combined with Halofuginone.
Etidronic acid
The risk or severity of jaw osteonecrosis and anti-angiogenesis can be increased when Halofuginone is combined with Etidronic acid.
Ibandronate
The risk or severity of jaw osteonecrosis and anti-angiogenesis can be increased when Halofuginone is combined with Ibandronate.
Incadronic acid
The risk or severity of jaw osteonecrosis and anti-angiogenesis can be increased when Halofuginone is combined with Incadronic acid.
Methoxy polyethylene glycol-epoetin beta
The risk or severity of Thrombosis can be increased when Methoxy polyethylene glycol-epoetin beta is combined with Halofuginone.
Pamidronic acid
The risk or severity of jaw osteonecrosis and anti-angiogenesis can be increased when Halofuginone is combined with Pamidronic acid.
Peginesatide
The risk or severity of Thrombosis can be increased when Peginesatide is combined with Halofuginone.
Risedronic acid
The risk or severity of jaw osteonecrosis and anti-angiogenesis can be increased when Halofuginone is combined with Risedronic acid.
Tiludronic acid
The risk or severity of jaw osteonecrosis and anti-angiogenesis can be increased when Halofuginone is combined with Tiludronic acid.
Zoledronic acid
The risk or severity of jaw osteonecrosis and anti-angiogenesis can be increased when Halofuginone is combined with Zoledronic acid.
3 References
  1. 1 . Elkin M, Miao HQ, Nagler A, Aingorn E, Reich R, Hemo I, Dou HL, Pines M, Vlodavsky I: Halofuginone: a potent inhibitor of critical steps in angiogenesis progression. FASEB J. 2000 Dec;14(15):2477-85.PubMed: 11099465
  2. 2 . Sundrud MS, Koralov SB, Feuerer M, Calado DP, Kozhaya AE, Rhule-Smith A, Lefebvre RE, Unutmaz D, Mazitschek R, Waldner H, Whitman M, Keller T, Rao A: Halofuginone inhibits TH17 cell differentiation by activating the amino acid starvation response. Science. 2009 Jun 5;324(5932):1334-8. doi: 10.1126/science.1172638.PubMed: 19498172
  3. 3 . Keller TL, Zocco D, Sundrud MS, Hendrick M, Edenius M, Yum J, Kim YJ, Lee HK, Cortese JF, Wirth DF, Dignam JD, Rao A, Yeo CY, Mazitschek R, Whitman M: Halofuginone and other febrifugine derivatives inhibit prolyl-tRNA synthetase. Nat Chem Biol. 2012 Feb 12;8(3):311-7. doi: 10.1038/nchembio.790.PubMed: 22327401