Pexidartinib

Identification

Summary

Pexidartinib is an antitumor agent that is used for the treatment of rare disease tenosynovial giant cell tumors (TGCT) by inhibiting colony-stimulating factor 1 and its receptor.

Brand Names

Turalio

Generic Name

Pexidartinib

DrugBank Accession Number

DB12978

Background

Pexidartinib is a selective tyrosine kinase inhibitor that works by inhibiting the colony-stimulating factor (CSF1)/CSF1 receptor pathway. Pexidartinib was originally developed by Daiichi Sankyo, Inc. and it was approved by the FDA in August 2019 as the first systemic therapy for adult patients with symptomatic tenosynovial giant cell tumor.¹¹ Tenosynovial giant cell tumor is a rare form of non-malignant tumor that causes the synovium and tendon sheaths to thicken and overgrow, leading to damage in surrounding joint tissue.^1,11 Debilitating symptoms often follow with tenosynovial giant cell tumors, along with a risk of significant functional limitations and a reduced quality of life in patients.¹¹

While surgical resection is a current standard of care for tenosynovial giant cell tumor, there are tumor types where surgeries are deemed clinically ineffective with a high risk of lifetime recurrence.¹⁰ Pexidartinib works by blocking the immune responses that are activated in tenosynovial giant cell tumors. In clinical trials, pexidartinib was shown to promote improvements in patient symptoms and functional outcomes in TGCT.² Pexidartinib is available in oral formulations and it is commonly marketed as Turalio.¹¹

Type

Small Molecule

Groups

Approved, Investigational

Structure

3D

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Similar Structures

Structure for Pexidartinib (DB12978)

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Weight

Average: 417.82
Monoisotopic: 417.0968077

Chemical Formula

C₂₀H₁₅ClF₃N₅

Synonyms

• Pexidartinib

External IDs

• CML-261
• PLX-3397
• PLX3397

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Pharmacology

Indication

Pexidartinib is indicated for the treatment of adult patients with symptomatic tenosynovial giant cell tumor (TGCT) associated with severe morbidity or functional limitations and not amenable to improvement with surgery.⁹

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Associated Conditions

Indication Type	Indication	Combined Product Details	Approval Level	Age Group	Patient Characteristics	Dose Form
Treatment of	Symptomatic tenosynovial giant cell tumor		••••••••••••	•••••	•••••••••••• •••••••••• •••••••••••• •• •••••••• •••••••••• ••••••••••	•••••••

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Contraindications & Blackbox Warnings

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Pharmacodynamics

Pexidartinib works by suppressing the growth of tenosynovial giant cell tumors. In clinical trials comprising of patients with symptomatic tenosynovial giant cell tumor, pexidartinib had a higher overall response rate, characterized by improved patient symptoms and functional outcomes, compared to placebo.² Pexidartinib works by inhibiting the activation and signaling of tumor-permissive cytokines and receptor tyrosine kinases that play a central role in tumor cell proliferation and survival.³ Taking pexidartinib with a high-fat meal may increase the incidence and severity of adverse reactions, including hepatotoxicity.¹²

Mechanism of action

Tenosynovial giant cell tumor is a rare, non-malignant neoplasm that causes abnormal growth and damage to the synovium, bursae, or tendon sheaths.¹¹ Recruitment of immune cells, specifically macrophages, is closely associated with the tumor mass formation in tenosynovial giant cell tumors. ¹ Macrophages drive tumor-promoting inflammation ⁷ and play a central role in every stage of tumor progression.⁶ As the most abundant immune cells in the tumor microenvironment of solid tumors, macrophages promote processes that enhance tumor survival, such as angiogenesis, tumor cell invasion, and intravasation at the primary site.⁶ They also modulate the immune response to tumors to inhibit tumor clearance and directly engage with tumor cells to activate pro-survival signaling pathways.⁸

The recruitment, proliferation, and irreversible differentiation of macrophages are regulated by colony-stimulating factor-1 (CSF-1),^3,5 which is a cytokine that is often translocated and highly expressed in tenosynovial giant cell tumors.⁸ Elevated expression of CSF-1 and CSF-1 receptor (CSF1R) has also been implicated in various models of malignant cancers and tumors.⁴ Pexidartinib targets the CSF1/CSF1R pathway as a selective CSF1R inhibitor. It stimulates the autoinhibited state of the CSF1R by interacting with the juxtamembrane region of CSF1R, which is responsible for folding and inactivation of the kinase domain, and preventing the binding of CSF1 and ATP to the region.¹ Without the binding of CSF1 to the receptor, CSF1R cannot undergo ligand-induced autophosphorylation.⁹ By inhibiting the CSF1R signaling pathway, pexidartinib works to inhibit tumor cell proliferation and downmodulate cells involved in the disease, such as macrophages. It was also shown to inhibit the CD117 or proto-oncogene receptor tyrosine kinase (cKIT), mutant fms-like tyrosine kinase 3 (FLT3), and platelet-derived growth factor receptor (PDGFR)-β, which are all receptor tyrosine kinases that regulate critical cellular processes such as cell proliferation and survival.³

Target	Actions	Organism
AMacrophage colony-stimulating factor 1 receptor	inhibitor	Humans
UMast/stem cell growth factor receptor Kit	inhibitor	Humans
UReceptor-type tyrosine-protein kinase FLT3	inhibitor	Humans
UPlatelet-derived growth factor receptor beta	inhibitor	Humans

Absorption

Following administration of single doses in healthy subjects and multiple doses in patients, the mean Cmax was 8625 ng/mL and the mean AUC was 77465 ngxh/mL. The median Tmax was 2.5 hours and the time to reach the steady state was approximately 7 days. Administration of pexidartinib with a high fat meal resulted in an increased drug Cmax and AUC by 100%, with a delay in Tmax by 2.5 hours.⁹

Volume of distribution

The apparent volume of distribution of pexidartinib is about 187 L.⁹ In rats, pexidartinib was shown to penetrate into the central nervous system.¹⁰

Protein binding

Based on the findings of in vitro plasma protein binding study, pexidartinib is about 99% bound to serum proteins, where it is extensively bound to human serum albumin by 99.9% and alpha-1-acid glycoprotein by 89.9%.⁹

Metabolism

Pexidartinib primarily undergoes oxidation mediated by hepatic CYP3A4 and glucuronidation by UGT1A4. Following UGT1A4-mediated glucuronidation, a major inactive N-glucuronide metabolite is formed with approximately 10% higher exposure than the parent drug after a single dose administration of pexidartinib.⁹ Based on the findings of in vitro studies, CYP1A2 and CYP2C9 may also play a minor role in drug metabolism.¹⁰

Route of elimination

Pexidartinib is predominantly excreted via feces, where fecal excretion accounts for 65% of total pexidartinib elimination. Via this route of elimination, about 44% of the compound found in feces is recovered as unchanged parent drug. The renal elimination accounts for 27% of pexidartinib elimination, where more than 10% of the compound is found as the N-glucuronide metabolite.⁹

Half-life

The elimination half-life is about 26.6 hours.⁹

Clearance

The apparent clearance is about 5.1 L/h.⁹

Adverse Effects

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Toxicity

There is limited human data on the overdose of pexidartinib. In 4-week toxicology studies, the no-observed-adverse-effect levels (NOAELs) of pexidatrtinib were determined to be 10 mg/kg/day in rats and 6 mg/kg/day in dogs.¹⁰ Pexidartinib was shown to cause hepatotoxicity in clinical trials, including mixed or cholestatic hepatotoxicity,² and embryo-fetal toxicity in animal studies.⁹

Pathways

Not Available

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Interactions

Drug Interactions Learn More" title="About Drug Interactions" id="structured-interactions-info" class="drug-info-popup" href="javascript:void(0);">

This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.

• Approved
• Vet approved
• Nutraceutical
• Illicit
• Withdrawn
• Investigational
• Experimental
• All Drugs

Drug	Interaction
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Abacavir	The metabolism of Abacavir can be decreased when combined with Pexidartinib.
Abatacept	The metabolism of Pexidartinib can be increased when combined with Abatacept.
Abemaciclib	The excretion of Abemaciclib can be decreased when combined with Pexidartinib.
Acalabrutinib	The metabolism of Pexidartinib can be decreased when combined with Acalabrutinib.
Acetaminophen	The metabolism of Pexidartinib can be increased when combined with Acetaminophen.

Food Interactions

• Avoid grapefruit products. Grapefruit inhibits CYP3A metabolism, which may increase the serum concentration of pexidartinib.
• Avoid St. John's Wort. This herb induces the CYP3A metabolism of pexidartinib and may reduce its serum concentration.
• Do not take with or immediately after a high-fat meal. Taking pexidartinib with a high-fat meal may increase incidence and severity of adverse reactions, including hepatotoxicity.
• Take on an empty stomach. Take at least 1 hour before or 2 hours after eating a meal or snack.
• Take separate from antacids. Take antacids at least 2 hours before or after pexidartinib.

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Product Ingredients

Ingredient	UNII	CAS	InChI Key
Pexidartinib hydrochloride	YS6WAI3XN7	2040295-03-0	CJLUYLRKLUYCEK-UHFFFAOYSA-N

Brand Name Prescription Products

Name	Dosage	Strength	Route	Labeller	Marketing Start	Marketing End	Region	Image
Turalio	Capsule	125 mg/1	Oral	Daiichi Sankyo, Inc.	2023-02-01	Not applicable
Turalio	Capsule	200 mg/1	Oral	Daiichi Sankyo Inc.	2019-08-02	2024-01-31

Categories

ATC Codes

L01EX15 — Pexidartinib

• L01EX — Other protein kinase inhibitors
• L01E — PROTEIN KINASE INHIBITORS
• L01 — ANTINEOPLASTIC AGENTS
• L — ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS

Drug Categories

• Amines
• Antineoplastic Agents
• Antineoplastic and Immunomodulating Agents
• Cancer immunotherapy
• Cytochrome P-450 CYP2B6 Inducers
• Cytochrome P-450 CYP2B6 Inducers (strength unknown)
• Cytochrome P-450 CYP2B6 Inhibitors
• Cytochrome P-450 CYP2B6 Inhibitors (strength unknown)
• Cytochrome P-450 CYP2C9 Inhibitors
• Cytochrome P-450 CYP2C9 Inhibitors (strength unknown)
• Cytochrome P-450 CYP3A Inducers
• Cytochrome P-450 CYP3A Inhibitors
• Cytochrome P-450 CYP3A Substrates
• Cytochrome P-450 CYP3A4 Inducers
• Cytochrome P-450 CYP3A4 Inducers (weak)
• Cytochrome P-450 CYP3A4 Inhibitors
• Cytochrome P-450 CYP3A4 Inhibitors (weak)
• Cytochrome P-450 CYP3A4 Substrates
• Cytochrome P-450 CYP3A4 Substrates with a Narrow Therapeutic Index
• Cytochrome P-450 Enzyme Inducers
• Cytochrome P-450 Enzyme Inhibitors
• Cytochrome P-450 Substrates
• Hepatotoxic Agents
• Immunotherapy
• Kinase Inhibitor
• MATE 1 Inhibitors
• MATE 2 Inhibitors
• MATE inhibitors
• Narrow Therapeutic Index Drugs
• OATP1B1/SLCO1B1 Inhibitors
• OATP1B3 inhibitors
• Organic Anion Transporting Polypeptide 2B1 Inhibitors
• Protein Kinase Inhibitors
• Pyridines
• Tyrosine Kinase Inhibitors
• UGT1A1 Inhibitors
• UGT1A4 substrates

Chemical TaxonomyProvided by Classyfire

Description

This compound belongs to the class of organic compounds known as pyrrolopyridines. These are compounds containing a pyrrolopyridine moiety, which consists of a pyrrole ring fused to a pyridine. Pyrrole is 5-membered ring consisting of four carbon atoms and one nitrogen atom. Pyridine is a 6-membered ring consisting of five carbon atoms and one nitrogen center.

Kingdom

Organic compounds

Super Class

Organoheterocyclic compounds

Class

Pyrrolopyridines

Sub Class

Not Available

Direct Parent

Pyrrolopyridines

Alternative Parents

Aminopyridines and derivatives / Substituted pyrroles / Imidolactams / Aryl chlorides / Heteroaromatic compounds / Azacyclic compounds / Organofluorides / Organochlorides / Hydrocarbon derivatives / Amines / Alkyl fluorides

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Substituents

Alkyl fluoride / Alkyl halide / Amine / Aminopyridine / Aromatic heteropolycyclic compound / Aryl chloride / Aryl halide / Azacycle / Heteroaromatic compound / Hydrocarbon derivative / Imidolactam / Organic nitrogen compound / Organochloride / Organofluoride / Organohalogen compound / Organonitrogen compound / Pyridine / Pyrrole / Pyrrolopyridine / Substituted pyrrole

show 10 more

Molecular Framework

Aromatic heteropolycyclic compounds

External Descriptors

Not Available

Affected organisms

• Humans and other mammals

Chemical Identifiers

UNII

6783M2LV5X

CAS number

1029044-16-3

InChI Key

JGWRKYUXBBNENE-UHFFFAOYSA-N

InChI

InChI=1S/C20H15ClF3N5/c21-15-6-16-14(10-28-19(16)29-11-15)5-12-2-4-18(26-7-12)27-9-13-1-3-17(25-8-13)20(22,23)24/h1-4,6-8,10-11H,5,9H2,(H,26,27)(H,28,29)

IUPAC Name

5-({5-chloro-1H-pyrrolo[2,3-b]pyridin-3-yl}methyl)-N-{[6-(trifluoromethyl)pyridin-3-yl]methyl}pyridin-2-amine

SMILES

FC(F)(F)C1=CC=C(CNC2=NC=C(CC3=CNC4=NC=C(Cl)C=C34)C=C2)C=N1

References

Synthesis Reference

Chen D, Zhang Y, Li J, Liu Y: Exploratory Process Development of Pexidartinib through the Tandem Tsuji–Trost Reaction and Heck Coupling. Synthesis. 2019 January 4;51(12):2564-2571. doi:10.1055/s-0037-1612421.

General References

1. Giustini N, Bernthal NM, Bukata SV, Singh AS: Tenosynovial giant cell tumor: case report of a patient effectively treated with pexidartinib (PLX3397) and review of the literature. Clin Sarcoma Res. 2018 Jul 10;8:14. doi: 10.1186/s13569-018-0101-2. eCollection 2018. [Article]
2. Tap WD, Gelderblom H, Palmerini E, Desai J, Bauer S, Blay JY, Alcindor T, Ganjoo K, Martin-Broto J, Ryan CW, Thomas DM, Peterfy C, Healey JH, van de Sande M, Gelhorn HL, Shuster DE, Wang Q, Yver A, Hsu HH, Lin PS, Tong-Starksen S, Stacchiotti S, Wagner AJ: Pexidartinib versus placebo for advanced tenosynovial giant cell tumour (ENLIVEN): a randomised phase 3 trial. Lancet. 2019 Jun 19. pii: S0140-6736(19)30764-0. doi: 10.1016/S0140-6736(19)30764-0. [Article]
3. Cannarile MA, Weisser M, Jacob W, Jegg AM, Ries CH, Ruttinger D: Colony-stimulating factor 1 receptor (CSF1R) inhibitors in cancer therapy. J Immunother Cancer. 2017 Jul 18;5(1):53. doi: 10.1186/s40425-017-0257-y. [Article]
4. Espinosa I, Beck AH, Lee CH, Zhu S, Montgomery KD, Marinelli RJ, Ganjoo KN, Nielsen TO, Gilks CB, West RB, van de Rijn M: Coordinate expression of colony-stimulating factor-1 and colony-stimulating factor-1-related proteins is associated with poor prognosis in gynecological and nongynecological leiomyosarcoma. Am J Pathol. 2009 Jun;174(6):2347-56. doi: 10.2353/ajpath.2009.081037. Epub 2009 May 14. [Article]
5. Hume DA, MacDonald KP: Therapeutic applications of macrophage colony-stimulating factor-1 (CSF-1) and antagonists of CSF-1 receptor (CSF-1R) signaling. Blood. 2012 Feb 23;119(8):1810-20. doi: 10.1182/blood-2011-09-379214. Epub 2011 Dec 20. [Article]
6. Nielsen SR, Schmid MC: Macrophages as Key Drivers of Cancer Progression and Metastasis. Mediators Inflamm. 2017;2017:9624760. doi: 10.1155/2017/9624760. Epub 2017 Jan 22. [Article]
7. Mantovani A, Marchesi F, Malesci A, Laghi L, Allavena P: Tumour-associated macrophages as treatment targets in oncology. Nat Rev Clin Oncol. 2017 Jul;14(7):399-416. doi: 10.1038/nrclinonc.2016.217. Epub 2017 Jan 24. [Article]
8. Cupp JS, Miller MA, Montgomery KD, Nielsen TO, O'Connell JX, Huntsman D, van de Rijn M, Gilks CB, West RB: Translocation and expression of CSF1 in pigmented villonodular synovitis, tenosynovial giant cell tumor, rheumatoid arthritis and other reactive synovitides. Am J Surg Pathol. 2007 Jun;31(6):970-6. doi: 10.1097/PAS.0b013e31802b86f8. [Article]
9. FDA Approved Drug Products: Turaliotm (pexidartinib) capsules [Link]
10. TURALIO (PEXIDARTINIB) CAPSULES - Daiichi Sankyo, Inc. - FDA Oncologic Drugs Advisory Committee Briefing Document [Link]
11. FDA approves first therapy for rare joint tumor - FDA News Release [Link]
12. FDA Approved Drug Products: Turaliotm (pexidartinib) capsules (October 2022) [Link]

External Links

Human Metabolome Database

HMDB0256360

PubChem Compound

25151352

PubChem Substance

347829117

ChemSpider

35308322

BindingDB

50177716

RxNav

2183102

ChEBI

145373

ChEMBL

CHEMBL3813873

ZINC

ZINC000115705166

PDBe Ligand

P31

Wikipedia

Pexidartinib

PDB Entries

4r7h / 7khg

Clinical Trials

Clinical Trials Learn More" title="About Clinical Trials" id="clinical-trials-info" class="drug-info-popup" href="javascript:void(0);">

Phase	Status	Purpose	Conditions	Count
4	Completed	Treatment	Tenosynovial Giant Cell Tumor	1
3	Active Not Recruiting	Treatment	Tenosynovial Giant Cell Tumor	1
3	Completed	Treatment	Giant Cell Tumor of Tendon Sheath / Pigmented Villonodular Synovitis / Tenosynovial Giant Cell Tumor	1
2	Completed	Treatment	Hodgkin's Lymphoma	1
2	Completed	Treatment	Malignant Melanoma	1

Pharmacoeconomics

Manufacturers

Not Available

Packagers

Not Available

Dosage Forms

Form	Route	Strength
Capsule	Oral	125 mg/1
Capsule	Oral	200 mg/1

Prices

Not Available

Patents

Patent Number	Pediatric Extension	Approved	Expires (estimated)	Region
US9358235	No	2016-06-07	2033-06-08
US8461169	No	2013-06-11	2028-04-19
US10189833	No	2019-01-29	2036-05-05
US9169250	No	2015-10-27	2027-11-21
US10435404	No	2019-10-08	2038-07-24
US8404700	No	2013-03-26	2027-11-21
US8722702	No	2014-05-13	2027-11-21
US7893075	No	2011-02-22	2028-10-13
US9802932	No	2017-10-31	2036-05-05
US10730876	No	2020-08-04	2036-05-05
US10941142	No	2021-03-09	2038-07-24
US10961240	No	2021-03-30	2038-07-24

Properties

State

Solid

Experimental Properties

Not Available

Predicted Properties

Property	Value	Source
Water Solubility	0.00315 mg/mL	ALOGPS
logP	4.64	ALOGPS
logP	4.54	Chemaxon
logS	-5.1	ALOGPS
pKa (Strongest Acidic)	15.68	Chemaxon
pKa (Strongest Basic)	6.76	Chemaxon
Physiological Charge	1	Chemaxon
Hydrogen Acceptor Count	4	Chemaxon
Hydrogen Donor Count	2	Chemaxon
Polar Surface Area	66.49 Å2	Chemaxon
Rotatable Bond Count	6	Chemaxon
Refractivity	105.89 m3·mol-1	Chemaxon
Polarizability	39.33 Å3	Chemaxon
Number of Rings	4	Chemaxon
Bioavailability	1	Chemaxon
Rule of Five	Yes	Chemaxon
Ghose Filter	Yes	Chemaxon
Veber's Rule	No	Chemaxon
MDDR-like Rule	Yes	Chemaxon

Predicted ADMET Features

Not Available

Spectra

Mass Spec (NIST)

Not Available

Spectra

Spectrum	Spectrum Type	Splash Key
Predicted MS/MS Spectrum - 10V, Positive (Annotated)	Predicted LC-MS/MS	splash10-014i-0000900000-9033d1be46655d0d7b3a
Predicted MS/MS Spectrum - 10V, Negative (Annotated)	Predicted LC-MS/MS	splash10-014i-3000900000-551e7dda2ae6dafe9b3d
Predicted MS/MS Spectrum - 20V, Positive (Annotated)	Predicted LC-MS/MS	splash10-014i-0003900000-ac37173bab41fe23aee9
Predicted MS/MS Spectrum - 20V, Negative (Annotated)	Predicted LC-MS/MS	splash10-0gc0-8504900000-7fb6ebe1c5e7b18ebbb3
Predicted MS/MS Spectrum - 40V, Positive (Annotated)	Predicted LC-MS/MS	splash10-03y0-0079100000-d2e6d0522405c8bbb4a3
Predicted MS/MS Spectrum - 40V, Negative (Annotated)	Predicted LC-MS/MS	splash10-0gc0-9655300000-af0f16fc28e7fafbf91e
Predicted 1H NMR Spectrum	1D NMR	Not Applicable
Predicted 13C NMR Spectrum	1D NMR	Not Applicable

Chromatographic Properties

Collision Cross Sections (CCS)

Adduct	CCS Value (Å2)	Source type	Source
[M-H]-	188.54614	predicted	DeepCCS 1.0 (2019)
[M+H]+	190.90414	predicted	DeepCCS 1.0 (2019)
[M+Na]+	197.53795	predicted	DeepCCS 1.0 (2019)

Targets

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insights and accelerate drug research.

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Details1. Macrophage colony-stimulating factor 1 receptor

Kind

Protein

Organism

Humans

Pharmacological action

Yes

Actions

Inhibitor

General Function

Protein homodimerization activity

Specific Function

Tyrosine-protein kinase that acts as cell-surface receptor for CSF1 and IL34 and plays an essential role in the regulation of survival, proliferation and differentiation of hematopoietic precursor ...

Gene Name

CSF1R

Uniprot ID

P07333

Uniprot Name

Macrophage colony-stimulating factor 1 receptor

Molecular Weight

107982.955 Da

References

1. Cannarile MA, Weisser M, Jacob W, Jegg AM, Ries CH, Ruttinger D: Colony-stimulating factor 1 receptor (CSF1R) inhibitors in cancer therapy. J Immunother Cancer. 2017 Jul 18;5(1):53. doi: 10.1186/s40425-017-0257-y. [Article]
2. FDA Approved Drug Products: Turaliotm (pexidartinib) capsules [Link]
3. TURALIO (PEXIDARTINIB) CAPSULES - Daiichi Sankyo, Inc. - FDA Oncologic Drugs Advisory Committee Briefing Document [Link]

Details2. Mast/stem cell growth factor receptor Kit

Kind

Protein

Organism

Humans

Pharmacological action

Unknown

Actions

Inhibitor

General Function

Transmembrane receptor protein tyrosine kinase activity

Specific Function

Tyrosine-protein kinase that acts as cell-surface receptor for the cytokine KITLG/SCF and plays an essential role in the regulation of cell survival and proliferation, hematopoiesis, stem cell main...

Gene Name

KIT

Uniprot ID

P10721

Uniprot Name

Mast/stem cell growth factor receptor Kit

Molecular Weight

109863.655 Da

References

1. Cannarile MA, Weisser M, Jacob W, Jegg AM, Ries CH, Ruttinger D: Colony-stimulating factor 1 receptor (CSF1R) inhibitors in cancer therapy. J Immunother Cancer. 2017 Jul 18;5(1):53. doi: 10.1186/s40425-017-0257-y. [Article]
2. TURALIO (PEXIDARTINIB) CAPSULES - Daiichi Sankyo, Inc. - FDA Oncologic Drugs Advisory Committee Briefing Document [Link]

Details3. Receptor-type tyrosine-protein kinase FLT3

Kind

Protein

Organism

Humans

Pharmacological action

Unknown

Actions

Inhibitor

General Function

Vascular endothelial growth factor-activated receptor activity

Specific Function

Tyrosine-protein kinase that acts as cell-surface receptor for the cytokine FLT3LG and regulates differentiation, proliferation and survival of hematopoietic progenitor cells and of dendritic cells...

Gene Name

FLT3

Uniprot ID

P36888

Uniprot Name

Receptor-type tyrosine-protein kinase FLT3

Molecular Weight

112902.51 Da

References

1. Cannarile MA, Weisser M, Jacob W, Jegg AM, Ries CH, Ruttinger D: Colony-stimulating factor 1 receptor (CSF1R) inhibitors in cancer therapy. J Immunother Cancer. 2017 Jul 18;5(1):53. doi: 10.1186/s40425-017-0257-y. [Article]
2. TURALIO (PEXIDARTINIB) CAPSULES - Daiichi Sankyo, Inc. - FDA Oncologic Drugs Advisory Committee Briefing Document [Link]

Details4. Platelet-derived growth factor receptor beta

Kind

Protein

Organism

Humans

Pharmacological action

Unknown

Actions

Inhibitor

General Function

Vascular endothelial growth factor binding

Specific Function

Tyrosine-protein kinase that acts as cell-surface receptor for homodimeric PDGFB and PDGFD and for heterodimers formed by PDGFA and PDGFB, and plays an essential role in the regulation of embryonic...

Gene Name

PDGFRB

Uniprot ID

P09619

Uniprot Name

Platelet-derived growth factor receptor beta

Molecular Weight

123966.895 Da

References

1. Cannarile MA, Weisser M, Jacob W, Jegg AM, Ries CH, Ruttinger D: Colony-stimulating factor 1 receptor (CSF1R) inhibitors in cancer therapy. J Immunother Cancer. 2017 Jul 18;5(1):53. doi: 10.1186/s40425-017-0257-y. [Article]
2. TURALIO (PEXIDARTINIB) CAPSULES - Daiichi Sankyo, Inc. - FDA Oncologic Drugs Advisory Committee Briefing Document [Link]

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Drug created at October 21, 2016 01:45 / Updated at December 01, 2022 11:28