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Giant cell tumors of the tendon sheath

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Unknown

2,578

Pain

614

Cancer

592

Hypertension

567

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Development Status

US Approved Rx

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Primary Target

Cell division cycle 2-like protein kinase 6

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Macrophage colony stimulating factor receptor

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Stem cell growth factor receptor

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Tyrosine-protein kinase receptor FLT3

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Vascular endothelial growth factor receptor 2

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Phase III

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Plexxikon

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PEXIDARTINIB

6783M2LV5X

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Status:

US Approved Rx (2019)

First approved in 2019

Class (Stereo):

CHEMICAL (ACHIRAL)

Targets:

Tyrosine-protein kinase receptor FLT3

Stem cell growth factor receptor

Cell division cycle 2-like protein kinase 6

Vascular endothelial growth factor receptor 2

Macrophage colony stimulating factor receptor

Conditions:

Pigmented villonodular synovitis

Tenosynovial giant cell tumor

Giant cell tumors of the tendon sheath

Pexidartinib (PLX3397) is a small-molecule receptor tyrosine kinase (RTK) inhibitor with potential antineoplastic activity. Pexidartinib binds to and inhibits phosphorylation of stem cell factor receptor (KIT), colony-stimulating factor-1 receptor (C...

SF1R) and FMS-like tyrosine kinase 3 (FLT3), which may result in the inhibition of tumor cell proliferation and down-modulation of macrophages, osteoclasts and mast cells involved in the osteolytic metastatic disease. FDA has granted Breakthrough Therapy Designation to pexidartinib (PLX3397) for the treatment of tenosynovial giant cell tumor (TGCT) where surgical removal of the tumor would be associated with potentially worsening functional limitation or severe morbidity. In addition to Breakthrough Therapy Designation, pexidartinib (PLX3397) has been granted Orphan Drug Designation by FDA for the treatment of pigmented villonodular synovitis (PVNS) and giant cell tumor of the tendon sheath (GCT-TS). It also has received Orphan Designation from the European Commission for the treatment of TGCT.

PEXIDARTINIB HYDROCHLORIDE

YS6WAI3XN7

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Search for Structure

Status:

US Approved Rx (2019)

First approved in 2019

Class (Stereo):

CHEMICAL (ACHIRAL)

Targets:

Tyrosine-protein kinase receptor FLT3

Stem cell growth factor receptor

Cell division cycle 2-like protein kinase 6

Vascular endothelial growth factor receptor 2

Macrophage colony stimulating factor receptor

Conditions:

Pigmented villonodular synovitis

Tenosynovial giant cell tumor

Giant cell tumors of the tendon sheath

Pexidartinib (PLX3397) is a small-molecule receptor tyrosine kinase (RTK) inhibitor with potential antineoplastic activity. Pexidartinib binds to and inhibits phosphorylation of stem cell factor receptor (KIT), colony-stimulating factor-1 receptor (C...

SF1R) and FMS-like tyrosine kinase 3 (FLT3), which may result in the inhibition of tumor cell proliferation and down-modulation of macrophages, osteoclasts and mast cells involved in the osteolytic metastatic disease. FDA has granted Breakthrough Therapy Designation to pexidartinib (PLX3397) for the treatment of tenosynovial giant cell tumor (TGCT) where surgical removal of the tumor would be associated with potentially worsening functional limitation or severe morbidity. In addition to Breakthrough Therapy Designation, pexidartinib (PLX3397) has been granted Orphan Drug Designation by FDA for the treatment of pigmented villonodular synovitis (PVNS) and giant cell tumor of the tendon sheath (GCT-TS). It also has received Orphan Designation from the European Commission for the treatment of TGCT.

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