imatinib

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Associated Genetic Biomarkers

Associated Diseases

Overview

Generic Name(s):

imatinib

Trade Name(s):

Gleevec

NCI Definition [1]:

An antineoplastic agent that inhibits the Bcr-Abl fusion protein tyrosine kinase, an abnormal enzyme produced by chronic myeloid leukemia cells that contain the Philadelphia chromosome. Imatinib also inhibits the receptor tyrosine kinases for platelet-derived growth factor (PDGF) and stem cell factor (SCF)/c-kit; the SCF/c-kit receptor tyrosine kinase is activated in gastrointestinal stromal tumor (GIST). This agent inhibits proliferation and induces apoptosis in cells that overexpress these oncoproteins.

Biomarker-Directed Therapies

Imatinib can be used in the treatment of gastrointestinal stromal tumor, melanoma, chronic myeloid leukemia, thymic carcinoma, and acute lymphoblastic leukemia. KIT, ABL1, and BCR are the most frequent biomarker inclusion criteria for use of imatinib [2].

Acute Lymphoblastic Leukemia +

Disease is predicted to be sensitive to imatinib: -

Biomarker Criteria:

Sample must match all of the following:

BCR-ABL1 Fusion

Clinical Setting(s): Refractory (FDA), Relapse (FDA)

Biomarker Criteria:

Sample must match all of the following:

BCR-ABL1 Fusion

Clinical Setting(s): Refractory (FDA), Relapse (FDA)

Disease is predicted to be resistant to imatinib: -

Biomarker Criteria:

Sample must match all of the following:

Sample must match one or more of the following:

BCR-ABL1 Resistance Mutations in CML (Imatinib)

Sample must match all of the following:

BCR-ABL1 Fusion

Clinical Setting(s): Refractory (NCCN)

Biomarker Criteria:

Sample must match all of the following:

Sample must match one or more of the following:

BCR-ABL1 Resistance Mutations in CML (Imatinib)

Sample must match all of the following:

BCR-ABL1 Fusion

Clinical Setting(s): Refractory (NCCN)

Chronic Myeloid Leukemia +

Disease is predicted to be sensitive to imatinib: -

Biomarker Criteria:

Sample must match all of the following:

BCR-ABL1 Fusion

Clinical Setting(s): Treatment Induction (FDA, NCCN)

Biomarker Criteria:

Sample must match all of the following:

BCR-ABL1 Fusion

Clinical Setting(s): Treatment Induction (FDA, NCCN)

Biomarker Criteria:

Sample must match all of the following:

BCR-ABL1 Fusion

Clinical Setting(s): Treatment Induction (NICE, BNF, SMC)

Biomarker Criteria:

Sample must match all of the following:

BCR-ABL1 Fusion

Clinical Setting(s): Treatment Induction (NICE, BNF, SMC)

Disease is predicted to be resistant to imatinib: -

Biomarker Criteria:

Sample must match all of the following:

Sample must match one or more of the following:

BCR-ABL1 Resistance Mutations in CML (Imatinib)

Sample must match all of the following:

BCR-ABL1 Fusion

Clinical Setting(s): Refractory (NCCN)

Biomarker Criteria:

Sample must match all of the following:

Sample must match one or more of the following:

BCR-ABL1 Resistance Mutations in CML (Imatinib)

Sample must match all of the following:

BCR-ABL1 Fusion

Clinical Setting(s): Refractory (NCCN)

Gastrointestinal Stromal Tumor +

Disease is predicted to be sensitive to imatinib: -

Biomarker Criteria:

Sample must match one or more of the following:

KIT Expression

Clinical Setting(s): Metastatic (FDA)

Note: Imatinib is indicated for patients with Kit (CD117) positive unresectable and/or metastatic malignant gastrointestinal stromal tumors (GIST).

Biomarker Criteria: Sample must match one or more of the following: KIT Expression	Clinical Setting(s): Metastatic (FDA)
	Note: Imatinib is indicated for patients with Kit (CD117) positive unresectable and/or metastatic malignant gastrointestinal stromal tumors (GIST).

Biomarker Criteria:

Sample must match all of the following:

KIT Exon 11 Mutation

Clinical Setting(s): Metastatic (NCCN)

Biomarker Criteria:

Sample must match all of the following:

KIT Exon 11 Mutation

Clinical Setting(s): Metastatic (NCCN)

Biomarker Criteria:

Sample must match all of the following:

Sample must match one or more of the following:

PDGFRA Mutation

Sample must not match any of the following:

PDGFRA D842V

Clinical Setting(s): Metastatic (NCCN)

Biomarker Criteria:

Sample must match all of the following:

Sample must match one or more of the following:

PDGFRA Mutation

Sample must not match any of the following:

PDGFRA D842V

Clinical Setting(s): Metastatic (NCCN)

Biomarker Criteria:

Sample must match all of the following:

KIT Exon 9 Mutation

Clinical Setting(s): Metastatic (NCCN)

Note: Confers intermediate sensitivity; Higher doses of imatinib may be more effective.

Biomarker Criteria: Sample must match all of the following: KIT Exon 9 Mutation	Clinical Setting(s): Metastatic (NCCN)
	Note: Confers intermediate sensitivity; Higher doses of imatinib may be more effective.

Biomarker Criteria:

Sample must match all of the following:

KIT Expression

Clinical Setting(s): Adjuvant (NICE, BNF, SMC), Metastatic (NICE, BNF)

Biomarker Criteria:

Sample must match all of the following:

KIT Expression

Clinical Setting(s): Adjuvant (NICE, BNF, SMC), Metastatic (NICE, BNF)

Disease is predicted to be resistant to imatinib: -

Biomarker Criteria:

Sample must match all of the following:

BRAF V600E

Clinical Setting(s): Metastatic (NCCN)

Biomarker Criteria:

Sample must match all of the following:

BRAF V600E

Clinical Setting(s): Metastatic (NCCN)

Biomarker Criteria:

Sample must match all of the following:

PDGFRA D842V

Clinical Setting(s): Metastatic (NCCN)

Biomarker Criteria:

Sample must match all of the following:

PDGFRA D842V

Clinical Setting(s): Metastatic (NCCN)

Melanoma +

Disease is predicted to be sensitive to imatinib: -

Biomarker Criteria:

Sample must match all of the following:

Sample must match one or more of the following:

KIT Mutation in Exon 9, 11, 13, 17, or 18

Sample must not match any of the following:

KIT A829P, KIT D816H, KIT D816V, KIT V654A

Clinical Setting(s): Metastatic (NCCN, MCG)

Biomarker Criteria:

Sample must match all of the following:

Sample must match one or more of the following:

KIT Mutation in Exon 9, 11, 13, 17, or 18

Sample must not match any of the following:

KIT A829P, KIT D816H, KIT D816V, KIT V654A

Clinical Setting(s): Metastatic (NCCN, MCG)

Biomarker Criteria:

Sample must match all of the following:

Sample must not match any of the following:

KIT D816H

Sample must match one or more of the following:

KIT K642E, KIT L576P, KIT V559A, KIT V559D, KIT W557R

Clinical Setting(s): Metastatic (MCG)

Biomarker Criteria:

Sample must match all of the following:

Sample must not match any of the following:

KIT D816H

Sample must match one or more of the following:

KIT K642E, KIT L576P, KIT V559A, KIT V559D, KIT W557R

Clinical Setting(s): Metastatic (MCG)

Disease is predicted to be resistant to imatinib: -

Biomarker Criteria:

Sample must match all of the following:

KIT Amplification

Clinical Setting(s): Metastatic (NCCN)

Biomarker Criteria:

Sample must match all of the following:

KIT Amplification

Clinical Setting(s): Metastatic (NCCN)

Biomarker Criteria:

Sample must match one or more of the following:

KIT A829P, KIT D816H, KIT D816V, KIT V654A

Clinical Setting(s): Metastatic (MCG)

Biomarker Criteria:

Sample must match one or more of the following:

KIT A829P, KIT D816H, KIT D816V, KIT V654A

Clinical Setting(s): Metastatic (MCG)

Myelodysplastic/Myeloproliferative Neoplasm +

Disease is predicted to be sensitive to imatinib: -

Biomarker Criteria:

Sample must match all of the following:

Sample must match one or more of the following:

PDGFR Fusions

Sample must not match any of the following:

BCR-ABL1 Fusion

Clinical Setting(s): First Line of Therapy (FDA, NCCN)

Note: Indicated for adult patients with myelodysplastic/myeloproliferative diseases (MDS/MPD) associated with PDGFR (platelet-derived growth factor receptor) gene re-arrangements.

Biomarker Criteria: Sample must match all of the following: Sample must match one or more of the following: PDGFR Fusions Sample must not match any of the following: BCR-ABL1 Fusion	Clinical Setting(s): First Line of Therapy (FDA, NCCN)
	Note: Indicated for adult patients with myelodysplastic/myeloproliferative diseases (MDS/MPD) associated with PDGFR (platelet-derived growth factor receptor) gene re-arrangements.

Biomarker Criteria:

Sample must match all of the following:

Sample must match one or more of the following:

PDGFR Fusions

Sample must not match any of the following:

BCR-ABL1 Fusion

Clinical Setting(s): First Line of Therapy (BNF)

Note: Indicated for adult patients with myelodysplastic/myeloproliferative diseases (MDS/MPD) associated with PDGFR (platelet-derived growth factor receptor) gene re-arrangements.

Biomarker Criteria: Sample must match all of the following: Sample must match one or more of the following: PDGFR Fusions Sample must not match any of the following: BCR-ABL1 Fusion	Clinical Setting(s): First Line of Therapy (BNF)
	Note: Indicated for adult patients with myelodysplastic/myeloproliferative diseases (MDS/MPD) associated with PDGFR (platelet-derived growth factor receptor) gene re-arrangements.

Thymic Carcinoma +

Disease is predicted to be sensitive to imatinib: -

Biomarker Criteria:

Sample must match one or more of the following:

KIT E490K, KIT H697Y, KIT V559A, KIT W557R

Clinical Setting(s): Metastatic (MCG)

Biomarker Criteria:

Sample must match one or more of the following:

KIT E490K, KIT H697Y, KIT V559A, KIT W557R

Clinical Setting(s): Metastatic (MCG)

Biomarker Criteria:

Sample must match one or more of the following:

KIT L576P, KIT V560del, KIT Y553N

Clinical Setting(s): Metastatic (MCG)

Biomarker Criteria:

Sample must match one or more of the following:

KIT L576P, KIT V560del, KIT Y553N

Clinical Setting(s): Metastatic (MCG)

Disease is predicted to be resistant to imatinib: -

Biomarker Criteria:

Sample must match all of the following:

KIT D820E

Clinical Setting(s): Metastatic (MCG)

Biomarker Criteria:

Sample must match all of the following:

KIT D820E

Clinical Setting(s): Metastatic (MCG)

Clinical Trials

View Clinical Trials for imatinib

Imatinib has been investigated in 32 clinical trials, of which 31 are open and 1 is closed. Of the trials investigating imatinib, 3 are phase 1 (3 open), 5 are phase 1/phase 2 (5 open), 11 are phase 2 (10 open), 9 are phase 3 (9 open), 2 are phase 4 (2 open), and 2 are no phase specified (2 open).

BCR-ABL1 Fusion, t(9;22)(q34;q11), and KIT Mutation are the most frequent biomarker inclusion criteria for imatinib clinical trials.

Chronic myeloid leukemia, gastrointestinal stromal tumor, and acute lymphoblastic leukemia are the most common diseases being investigated in imatinib clinical trials [2].

Top Biomarker Inclusion Criteria for Open Clinical Trials Investigating Imatinib

Top Biomarker Inclusion Criteria for Closed Clinical Trials Investigating Imatinib

This graph displays the 20 most frequently occurring biomarkers curated on clinical trials investigating imatinib and the cancer types associated with these biomarkers. These numbers are derived from a set of 5,956 clinical trials for which biomarker status defines treatment.

Drug Details

Synonyms [2]:

sti-571, cgp57148, cgp57148b, imatinibum, imatinib (substance), alpha-(4-methyl-1-piperazinyl)-3'-((4-(3-pyridyl)-2-pyrimidinyl)amino)-p-toluidide, 4-(4-methyl-piperazin-1-ylmethyl)-n-[4-methyl-3-(4-pyridin-3-yl-pyrimidin-2-ylamino)-phenyl]-benzamide, 4-[(4-methyl-1-piperazinyl)methyl]-n-[4-methyl-3-[[4-(3-pyridinyl)-2-pyrimidinyl]amino]phenyl]benzamide, imatinib methansulfonate, imatinib, alpha-(4-methyl-1-piperazinyl)-3'-((4-(3-pyridyl)-2-pyrimidinyl)amino)-p-tolu-p-toluidide, imatinib (product), imatinib, Gleevec

Drug Categories [2]:

ABL inhibitors, Tyrosine kinase inhibitors

Drug Target(s) [2]:

ABL1, ABL2, DDR1, KIT, PDGFRA

NCIT ID [1]:

C1687

SNOMED ID [1]:

F-61F79

References

1. National Cancer Institute. NCI Thesaurus Version 18.11d. https://ncit.nci.nih.gov/ncitbrowser/. [2018-07-30] [2018-08-02].

2. All assertions and clinical trial landscape data are curated from primary sources. You can read more about the curation process here.

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Associated Genetic Biomarkers

Associated Diseases

Overview

Biomarker-Directed Therapies

Clinical Trials

Drug Details

References

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