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Targeted Cancer Therapies

Targeted Cancer Therapies

The targeted cancer therapies, also known as “molecular targeted therapies,” take advantage of the molecular and genetic differences between the cancer cells and the normal cells. It needs a thorough understanding of the cancer cells to develop drugs that can target specific molecular aspects that drive the growth, progression, and spread of cancer cells without affecting the growth and survival of other normal cells in the body.
There are several types of targeted therapies against specific...

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Related Experiment Video

Updated: Jul 15, 2026

Next Generation Sequencing for the Detection of Actionable Mutations in Solid and Liquid Tumors

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Published on: September 20, 2016

Structure-Based Design and Identification of FT-2102 (Olutasidenib), a Potent Mutant-Selective IDH1 Inhibitor.

Justin A Caravella¹, Jian Lin¹, R Bruce Diebold¹

¹FORMA Therapeutics, Inc. , 500 Arsenal Street, Suite 100 , Watertown , Massachusetts 02472 , United States.

Journal of Medicinal Chemistry

|January 24, 2020

Summary

Researchers developed FT-2102, a potent inhibitor targeting mutant IDH1 (mIDH1) in cancer. This orally available drug shows promise for treating various cancers, including gliomas, by reducing tumor-promoting metabolites.

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Testing Targeted Therapies in Cancer using Structural DNA Alteration Analysis and Patient-Derived Xenografts

Testing Targeted Therapies in Cancer using Structural DNA Alteration Analysis and Patient-Derived Xenografts

Published on: July 25, 2020

Area of Science:

Oncology
Medicinal Chemistry
Pharmacology

Background:

Mutant IDH1 (mIDH1) is a driver in certain cancers.
Targeting mIDH1 is a promising therapeutic strategy.
Existing inhibitors may lack optimal properties for broad clinical use.

Purpose of the Study:

To design and optimize a novel, potent, and selective mIDH1 inhibitor.
To identify a drug candidate with favorable oral bioavailability and brain penetrance.
To evaluate the efficacy of the novel inhibitor in preclinical models.

Main Methods:

Structure-based drug design of quinoline-based compounds.
Lead optimization focusing on potency, selectivity, and pharmacokinetic properties.
In vivo evaluation in mIDH1 xenograft tumor models to assess 2-hydroxyglutarate reduction.

Main Results:

Identification of FT-2102, a potent and selective mIDH1 inhibitor.
FT-2102 exhibits excellent ADME/PK properties and brain penetrance.
Significant reduction of 2-hydroxyglutarate levels observed in xenograft models.

Conclusions:

FT-2102 is a promising drug candidate for mIDH1-driven cancers.
The compound's properties support its clinical development.
Potential applications include hematologic malignancies, solid tumors, and gliomas.