Midostaurin

Identification

Summary

Midostaurin is an antineoplastic agent used to treat high-risk acute myeloid leukemia (AML) with specific mutations, aggressive systemic mastocytosis (ASM), systemic mastocytosis with associated hematologic neoplasm (SM-AHN), or mast cell leukemia (MCL).

Brand Names

Rydapt

Generic Name

Midostaurin

DrugBank Accession Number

DB06595

Background

Midostaurin (as Rydapt) is a multitarget kinase inhibitor for the treatment for adult patients with newly diagnosed acute myeloid leukemia (AML) who have a specific genetic mutation called FLT3. It was initially characterized as a potential broad-spectrum antineoplastic agent, with activity toward diverse solid and hematopoietic tumors ⁴. It was approved on April 28, 2017 and has shown to increase the overall survival rate in patients with AML as an adjunct therapy along with chemotherapeutic agents.

Type

Small Molecule

Groups

Approved, Investigational

Structure

3D

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MOLSDF3D-SDFPDBSMILESInChI

Similar Structures

Structure for Midostaurin (DB06595)

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Weight

Average: 570.649
Monoisotopic: 570.226705462

Chemical Formula

C₃₅H₃₀N₄O₄

Synonyms

• 4'-N-benzoylstaurosporine
• Midostaurin

External IDs

• CGP 41251
• CGP-41251
• NVP-PKC412
• PKC 412
• PKC-412

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Pharmacology

Indication

Investigated for use/treatment in adult patients with high-risk acute myeloid leukemia (AML) who are FLT3 mutation-positive, agressive systemic mastocytosis (ASM), systemic mastocytosis with associated hematological neoplasm (SM-AHN), or mast cell leukemia (MCL).

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Associated Conditions

Indication Type	Indication	Combined Product Details	Approval Level	Age Group	Patient Characteristics	Dose Form
Used in combination to treat	Acute myeloid leukemia	Regimen in combination with: Daunorubicin (DB00694), Cytarabine (DB00987)	••••••••••••
Treatment of	Aggressive systemic mastocytosis		••••••••••••
Treatment of	Mast cell leukemia		••••••••••••
Treatment of	Systemic mastocytosis		••••••••••••

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Contraindications & Blackbox Warnings

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Pharmacodynamics

It targets multiple WT and mutated kinases that, when activated, constitutively stimulate aberrant signalling cascades that lead to malignancies such as AML and ASM. Alternative pharmacodynamic effect of midostaurin in prolonging QTc intervals was not clinically significant in patients with advanced SM or AML when compared to placebo. Midostaurin is therapeutically beneficial as a combination therapy for patients undergoing chemotherapy.

Mechanism of action

It potently inhibits multiple receptor tyrosine kinases. Midostaurin and its major active metabolites CGP62221 and CGP52421 inhibit the activity of protein kinase C alpha (PKCalpha), VEGFR2, KIT, PDGFR and WT and/or mutant FLT3 tyrosine kinases. Inhibition of FLT3 receptor signalling cascades induces apoptosis of target leukemia cells expressing target receptors and mast cells, in addition to its antiproliferative activity toward multiple cancer cell lines ⁴. Midostaurin also interacts with organic anion transporter (OATP) 1A1 and multidrug resistance protein (MRP)-2 according to preliminary in vitro studies.

Target	Actions	Organism
AProtein kinase C alpha type	antagonist inhibitor	Humans
AVascular endothelial growth factor receptor 2	antagonist inhibitor	Humans
APlatelet-derived growth factor receptor alpha	antagonist inhibitor	Humans
APlatelet-derived growth factor receptor beta	antagonist inhibitor	Humans
AReceptor-type tyrosine-protein kinase FLT3	antagonist inhibitor	Humans
UMast/stem cell growth factor receptor Kit	antagonist inhibitor	Humans

Absorption

The time to reach maximum concentration ranges from 1-3 hrs in fasting patients. The maximum concentration and the time it takes to reach this concentration is reduced up to 20% in presence of a standard meal.

Volume of distribution

The Vd of midostaurin is 95.2L. The parent drug and its main metabolites (CGP62221, CGP52421) are distributed in plasma in vitro.

Protein binding

Midostaurin predominantly binds to α1-acid glycoprotein in vitro. The parent drug and its metabolites are >99.8% bound to plasma proteins in vitro.

Metabolism

Midostaurin is primarily metabolized into CGP62221 and CGP52421 via hepatic CYP3A4 enzymatic activity. The metabolism of CGP62221 takes place initially in a linear relationship whereas CGP52421 formation is an inducible process ⁵.

Hover over products below to view reaction partners

• Midostaurin
  • CGP 52421
  • CGP 62221

Route of elimination

Accounting for 95% of recovered dose eliminated through fecal excretion, 91% was determined as metabolites and 4% as unchanged parent drug. Remaining 5% of the recovered dose is eliminated via renal excretion.

Half-life

Elimination half life is approximately 21 hrs for midostaurin, 32 hrs for CGP62221 and 482 hrs for CGP52421.

Clearance

The clearance values of during the initial formation of metabolites are 1.47 L/h for CGP62221 metabolite and 0.501 L/h for CGP52421. 28 days following the oral administration of midostaurin, the clearance of CGP52421 may increase up to 5.2 fold in a recommended dose of 25 mg, resulting in a 2.1- to 2.5-fold increase in total clearance of midostaurin ⁵.

Adverse Effects

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Toxicity

In a fertility study involving female and male rats, there is evidence of reproductive toxicity including reduced sperm count and decline pregnancy rates when administering 0.01 to 0.1 times the recommended dose in humans. LD50 for oral midostaurin for mouse, rat and rabbit are 300mg/kg, 980mg/kg and 3200mg/kg, respectively ⁸. Incidences of pulmonary toxicities including interstitial lung disease and pneumonitis have occured in few patients undergoing midostaurin monotherapy or combination therapy.

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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1,2-Benzodiazepine	The metabolism of 1,2-Benzodiazepine can be decreased when combined with Midostaurin.
Abametapir	The serum concentration of Midostaurin can be increased when it is combined with Abametapir.
Abatacept	The metabolism of Midostaurin can be increased when combined with Abatacept.
Abemaciclib	The metabolism of Abemaciclib can be decreased when combined with Midostaurin.
Abiraterone	The metabolism of Abiraterone can be increased when combined with Midostaurin.

Food Interactions

• Avoid St. John's Wort. This herb induces the CYP3A4 metabolism of midostaurin and may reduce its serum concentration.
• Exercise caution with grapefruit products. Grapefruit inhibits the CYP3A4 metabolism of midostaurin, which may increase its serum concentration.
• Take with food. Taking midostaurin with food increases the AUC, but it also prolongs the Tmax and reduces Cmax.

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Brand Name Prescription Products

Name	Dosage	Strength	Route	Labeller	Marketing Start	Marketing End	Region	Image
Rydapt	Capsule, liquid filled	25 mg/1	Oral	Novartis Pharmaceuticals Corporation	2017-04-28	Not applicable
Rydapt	Capsule	25 mg	Oral	Novartis Europharm Limited	2020-12-16	Not applicable
Rydapt	Capsule	25 mg	Oral	Novartis Europharm Limited	2020-12-16	Not applicable
Rydapt	Capsule	25 mg	Oral	Novartis	2017-09-08	Not applicable

Categories

ATC Codes

L01EX10 — Midostaurin

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

Drug Categories

• Alkaloids
• Antineoplastic Agents
• Antineoplastic and Immunomodulating Agents
• Carbazoles
• Cytochrome P-450 CYP1A2 Inducers
• Cytochrome P-450 CYP1A2 Inducers (strength unknown)
• Cytochrome P-450 CYP1A2 Inhibitors
• Cytochrome P-450 CYP1A2 Inhibitors (strong)
• Cytochrome P-450 CYP2B6 Inducers
• Cytochrome P-450 CYP2B6 Inducers (strength unknown)
• Cytochrome P-450 CYP2C19 Inducers
• Cytochrome P-450 CYP2C19 Inducers (strength unknown)
• Cytochrome P-450 CYP2C19 Inhibitors
• Cytochrome P-450 CYP2C19 Inhibitors (weak)
• Cytochrome P-450 CYP2C8 Inducers
• Cytochrome P-450 CYP2C8 Inducers (strength unknown)
• Cytochrome P-450 CYP2C8 Inhibitors
• Cytochrome P-450 CYP2C8 Inhibitors (strength unknown)
• Cytochrome P-450 CYP2C9 Inducers
• Cytochrome P-450 CYP2C9 Inducers (strength unknown)
• Cytochrome P-450 CYP2C9 Inhibitors
• Cytochrome P-450 CYP2C9 Inhibitors (strength unknown)
• Cytochrome P-450 CYP2D6 Inhibitors
• Cytochrome P-450 CYP2D6 Inhibitors (strong)
• Cytochrome P-450 CYP2E1 Inhibitors
• Cytochrome P-450 CYP2E1 Inhibitors (strong)
• Cytochrome P-450 CYP3A Inducers
• Cytochrome P-450 CYP3A Inducers (strong)
• Cytochrome P-450 CYP3A Inhibitors
• Cytochrome P-450 CYP3A Substrates
• Cytochrome P-450 CYP3A4 Inducers
• Cytochrome P-450 CYP3A4 Inducers (strength unknown)
• Cytochrome P-450 CYP3A4 Inducers (strong)
• Cytochrome P-450 CYP3A4 Inhibitors
• Cytochrome P-450 CYP3A4 Inhibitors (strong)
• Cytochrome P-450 CYP3A4 Substrates
• Cytochrome P-450 CYP3A4 Substrates with a Narrow Therapeutic Index
• Cytochrome P-450 CYP3A5 Inducers
• Cytochrome P-450 CYP3A5 Inducers (strength unknown)
• Cytochrome P-450 CYP3A7 Inducers
• Cytochrome P-450 CYP3A7 Inducers (strength unknown)
• Cytochrome P-450 Enzyme Inducers
• Cytochrome P-450 Enzyme Inhibitors
• Cytochrome P-450 Substrates
• Enzyme Inhibitors
• Heterocyclic Compounds, Fused-Ring
• Indole Alkaloids
• Indoles
• Indolizidines
• Indolizines
• Kinase Inhibitor
• Narrow Therapeutic Index Drugs
• Protein Kinase C, antagonists & inhibitors
• Protein Kinase Inhibitors
• Receptor Tyrosine Kinase Inhibitors
• Tyrosine Kinase Inhibitors

Chemical TaxonomyProvided by Classyfire

Description

This compound belongs to the class of organic compounds known as indolocarbazoles. These are polycyclic aromatic compounds containing an indole fused to a carbazole.

Kingdom

Organic compounds

Super Class

Organoheterocyclic compounds

Class

Indoles and derivatives

Sub Class

Carbazoles

Direct Parent

Indolocarbazoles

Alternative Parents

Pyrrolo[2,3-a]carbazoles / Pyrroloindoles / Isoindolones / Benzamides / Indoles / Benzoyl derivatives / Oxanes / Tertiary carboxylic acid amides / Heteroaromatic compounds / Pyrroles / Lactams / Secondary carboxylic acid amides / Oxacyclic compounds / Azacyclic compounds / Dialkyl ethers / Hydrocarbon derivatives / Organic oxides / Organonitrogen compounds / Organopnictogen compounds

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Substituents

Aromatic heteropolycyclic compound / Azacycle / Benzamide / Benzenoid / Benzoic acid or derivatives / Benzoyl / Carboxamide group / Carboxylic acid derivative / Dialkyl ether / Ether / Heteroaromatic compound / Hydrocarbon derivative / Indole / Indolocarbazole / Isoindole or derivatives / Isoindoline / Isoindolone / Lactam / Monocyclic benzene moiety / Organic nitrogen compound / Organic oxide / Organic oxygen compound / Organonitrogen compound / Organooxygen compound / Organopnictogen compound / Oxacycle / Oxane / Pyrrole / Pyrrolo[2,3-a]carbazole / Pyrroloindole / Secondary carboxylic acid amide / Tertiary carboxylic acid amide

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Molecular Framework

Aromatic heteropolycyclic compounds

External Descriptors

benzamides, gamma-lactam, organic heterooctacyclic compound, indolocarbazole (CHEBI:63452)

Affected organisms

• Humans and other mammals

Chemical Identifiers

UNII

ID912S5VON

CAS number

120685-11-2

InChI Key

BMGQWWVMWDBQGC-IIFHNQTCSA-N

InChI

InChI=1S/C35H30N4O4/c1-35-32(42-3)25(37(2)34(41)19-11-5-4-6-12-19)17-26(43-35)38-23-15-9-7-13-20(23)28-29-22(18-36-33(29)40)27-21-14-8-10-16-24(21)39(35)31(27)30(28)38/h4-16,25-26,32H,17-18H2,1-3H3,(H,36,40)/t25-,26-,32-,35+/m1/s1

IUPAC Name

N-[(2S,3R,4R,6R)-3-methoxy-2-methyl-16-oxo-29-oxa-1,7,17-triazaoctacyclo[12.12.2.1^{2,6}.0^{7,28}.0^{8,13}.0^{15,19}.0^{20,27}.0^{21,26}]nonacosa-8(13),9,11,14(28),15(19),20(27),21(26),22,24-nonaen-4-yl]-N-methylbenzamide

SMILES

CO[C@@H]1[C@@H](C[C@H]2O[C@]1(C)N1C3=C(C=CC=C3)C3=C1C1=C(C4=C(C=CC=C4)N21)C1=C3CNC1=O)N(C)C(=O)C1=CC=CC=C1

References

General References

1. Fischer T, Stone RM, Deangelo DJ, Galinsky I, Estey E, Lanza C, Fox E, Ehninger G, Feldman EJ, Schiller GJ, Klimek VM, Nimer SD, Gilliland DG, Dutreix C, Huntsman-Labed A, Virkus J, Giles FJ: Phase IIB trial of oral Midostaurin (PKC412), the FMS-like tyrosine kinase 3 receptor (FLT3) and multi-targeted kinase inhibitor, in patients with acute myeloid leukemia and high-risk myelodysplastic syndrome with either wild-type or mutated FLT3. J Clin Oncol. 2010 Oct 1;28(28):4339-45. doi: 10.1200/JCO.2010.28.9678. Epub 2010 Aug 23. [Article]
2. Millward MJ, House C, Bowtell D, Webster L, Olver IN, Gore M, Copeman M, Lynch K, Yap A, Wang Y, Cohen PS, Zalcberg J: The multikinase inhibitor midostaurin (PKC412A) lacks activity in metastatic melanoma: a phase IIA clinical and biologic study. Br J Cancer. 2006 Oct 9;95(7):829-34. Epub 2006 Sep 12. [Article]
3. Gotlib J, Kluin-Nelemans HC, George TI, Akin C, Sotlar K, Hermine O, Awan FT, Hexner E, Mauro MJ, Sternberg DW, Villeneuve M, Huntsman Labed A, Stanek EJ, Hartmann K, Horny HP, Valent P, Reiter A: Efficacy and Safety of Midostaurin in Advanced Systemic Mastocytosis. N Engl J Med. 2016 Jun 30;374(26):2530-41. doi: 10.1056/NEJMoa1513098. [Article]
4. Gallogly MM, Lazarus HM: Midostaurin: an emerging treatment for acute myeloid leukemia patients. J Blood Med. 2016 Apr 19;7:73-83. doi: 10.2147/JBM.S100283. eCollection 2016. [Article]
5. Yin OQ, Wang Y, Schran H: A mechanism-based population pharmacokinetic model for characterizing time-dependent pharmacokinetics of midostaurin and its metabolites in human subjects. Clin Pharmacokinet. 2008;47(12):807-16. doi: 10.2165/0003088-200847120-00005. [Article]
6. Abmole Midostaurin MSDS [Link]
7. Alfa Aesar Midostaurin MSDS [Link]
8. Cayman Midostaurin MSDS [Link]
9. FDA Approved Drug Products: RYDAPT (midostaurin) capsules [Link]

External Links

KEGG Drug

D05029

PubChem Compound

9829523

PubChem Substance

347827778

ChemSpider

8005258

BindingDB

50326053

RxNav

1919083

ChEBI

63452

ChEMBL

CHEMBL608533

ZINC

ZINC000100013130

PDBe Ligand

2K2

Drugs.com

Drugs.com Drug Page

Wikipedia

Midostaurin

PDB Entries

4nct

FDA label

Download (306 KB)

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
3	Active Not Recruiting	Treatment	Acute Myeloid Leukemia / Myelodysplastic Syndrome With Excess Blasts-2 (MDS-EB-2)	1
3	Active Not Recruiting	Treatment	Leukemias	1
3	Completed	Treatment	Acute Myeloid Leukemia	2
3	Recruiting	Treatment	Acute Myeloid Leukemia With FMS-like Tyrosine Kinase (FLT3) / Internal Tandem Duplication (ITD) Mutation	1
3	Recruiting	Treatment	Newly Diagnosed FLT3 Mutated AML	1

Pharmacoeconomics

Manufacturers

Not Available

Packagers

Not Available

Dosage Forms

Form	Route	Strength
Capsule, liquid filled	Oral	25 mg/1
Capsule	Oral	25 mg
Capsule	Oral
Capsule, liquid filled	Oral	25 mg

Prices

Not Available

Patents

Patent Number	Pediatric Extension	Approved	Expires (estimated)	Region
US8575146	No	2013-11-05	2030-12-02
US7973031	No	2011-07-05	2024-10-17
US8222244	No	2012-07-17	2022-10-29

Properties

State

Solid

Experimental Properties

Property	Value	Source
melting point (°C)	235-260	Alfa Aesar MSDS
water solubility	<1mg/mL	Abmole MSDS
logP	5.89	Not Available

Predicted Properties

Property	Value	Source
Water Solubility	0.0157 mg/mL	ALOGPS
logP	4.52	ALOGPS
logP	5.43	Chemaxon
logS	-4.6	ALOGPS
pKa (Strongest Acidic)	13.45	Chemaxon
pKa (Strongest Basic)	-0.83	Chemaxon
Physiological Charge	0	Chemaxon
Hydrogen Acceptor Count	4	Chemaxon
Hydrogen Donor Count	1	Chemaxon
Polar Surface Area	77.73 Å2	Chemaxon
Rotatable Bond Count	3	Chemaxon
Refractivity	162.61 m3·mol-1	Chemaxon
Polarizability	60.58 Å3	Chemaxon
Number of Rings	9	Chemaxon
Bioavailability	0	Chemaxon
Rule of Five	No	Chemaxon
Ghose Filter	No	Chemaxon
Veber's Rule	No	Chemaxon
MDDR-like Rule	No	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	splash10-00xr-0300790000-4ec8d1577ca0af0055ee
Predicted MS/MS Spectrum - 10V, Negative (Annotated)	Predicted LC-MS/MS	splash10-014i-0000490000-a6791c7470f840aa0633
Predicted MS/MS Spectrum - 20V, Positive (Annotated)	Predicted LC-MS/MS	splash10-00di-0300390000-e6a8595808c298599bb7
Predicted MS/MS Spectrum - 20V, Negative (Annotated)	Predicted LC-MS/MS	splash10-017r-0000950000-2de28c7c76160139a545
Predicted MS/MS Spectrum - 40V, Positive (Annotated)	Predicted LC-MS/MS	splash10-0200-9704070000-02affb55aa78ab9123b6
Predicted MS/MS Spectrum - 40V, Negative (Annotated)	Predicted LC-MS/MS	splash10-0g29-4201940000-0e4157981d1b1ebe6112

Chromatographic Properties

Collision Cross Sections (CCS)

Adduct	CCS Value (Å2)	Source type	Source
[M-H]-	243.868	predicted	DeepCCS 1.0 (2019)
[M+H]+	245.76341	predicted	DeepCCS 1.0 (2019)
[M+Na]+	251.82526	predicted	DeepCCS 1.0 (2019)

Targets

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Details1. Protein kinase C alpha type

Kind

Protein

Organism

Humans

Pharmacological action

Yes

Actions

Antagonist

Inhibitor

General Function

Zinc ion binding

Specific Function

Calcium-activated, phospholipid- and diacylglycerol (DAG)-dependent serine/threonine-protein kinase that is involved in positive and negative regulation of cell proliferation, apoptosis, differenti...

Gene Name

PRKCA

Uniprot ID

P17252

Uniprot Name

Protein kinase C alpha type

Molecular Weight

76749.445 Da

References

1. Millward MJ, House C, Bowtell D, Webster L, Olver IN, Gore M, Copeman M, Lynch K, Yap A, Wang Y, Cohen PS, Zalcberg J: The multikinase inhibitor midostaurin (PKC412A) lacks activity in metastatic melanoma: a phase IIA clinical and biologic study. Br J Cancer. 2006 Oct 9;95(7):829-34. Epub 2006 Sep 12. [Article]

Details2. Vascular endothelial growth factor receptor 2

Kind

Protein

Organism

Humans

Pharmacological action

Yes

Actions

Antagonist

Inhibitor

General Function

Vascular endothelial growth factor-activated receptor activity

Specific Function

Tyrosine-protein kinase that acts as a cell-surface receptor for VEGFA, VEGFC and VEGFD. Plays an essential role in the regulation of angiogenesis, vascular development, vascular permeability, and ...

Gene Name

KDR

Uniprot ID

P35968

Uniprot Name

Vascular endothelial growth factor receptor 2

Molecular Weight

151525.555 Da

References

1. Millward MJ, House C, Bowtell D, Webster L, Olver IN, Gore M, Copeman M, Lynch K, Yap A, Wang Y, Cohen PS, Zalcberg J: The multikinase inhibitor midostaurin (PKC412A) lacks activity in metastatic melanoma: a phase IIA clinical and biologic study. Br J Cancer. 2006 Oct 9;95(7):829-34. Epub 2006 Sep 12. [Article]

Details3. Platelet-derived growth factor receptor alpha

Kind

Protein

Organism

Humans

Pharmacological action

Yes

Actions

Antagonist

Inhibitor

General Function

Vascular endothelial growth factor-activated receptor activity

Specific Function

Tyrosine-protein kinase that acts as a cell-surface receptor for PDGFA, PDGFB and PDGFC and plays an essential role in the regulation of embryonic development, cell proliferation, survival and chem...

Gene Name

PDGFRA

Uniprot ID

P16234

Uniprot Name

Platelet-derived growth factor receptor alpha

Molecular Weight

122668.46 Da

References

1. Millward MJ, House C, Bowtell D, Webster L, Olver IN, Gore M, Copeman M, Lynch K, Yap A, Wang Y, Cohen PS, Zalcberg J: The multikinase inhibitor midostaurin (PKC412A) lacks activity in metastatic melanoma: a phase IIA clinical and biologic study. Br J Cancer. 2006 Oct 9;95(7):829-34. Epub 2006 Sep 12. [Article]

Details4. Platelet-derived growth factor receptor beta

Kind

Protein

Organism

Humans

Pharmacological action

Yes

Actions

Antagonist

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. Millward MJ, House C, Bowtell D, Webster L, Olver IN, Gore M, Copeman M, Lynch K, Yap A, Wang Y, Cohen PS, Zalcberg J: The multikinase inhibitor midostaurin (PKC412A) lacks activity in metastatic melanoma: a phase IIA clinical and biologic study. Br J Cancer. 2006 Oct 9;95(7):829-34. Epub 2006 Sep 12. [Article]

Details5. Receptor-type tyrosine-protein kinase FLT3

Kind

Protein

Organism

Humans

Pharmacological action

Yes

Actions

Antagonist

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. Millward MJ, House C, Bowtell D, Webster L, Olver IN, Gore M, Copeman M, Lynch K, Yap A, Wang Y, Cohen PS, Zalcberg J: The multikinase inhibitor midostaurin (PKC412A) lacks activity in metastatic melanoma: a phase IIA clinical and biologic study. Br J Cancer. 2006 Oct 9;95(7):829-34. Epub 2006 Sep 12. [Article]
2. Gallogly MM, Lazarus HM: Midostaurin: an emerging treatment for acute myeloid leukemia patients. J Blood Med. 2016 Apr 19;7:73-83. doi: 10.2147/JBM.S100283. eCollection 2016. [Article]

Details6. Mast/stem cell growth factor receptor Kit

Kind

Protein

Organism

Humans

Pharmacological action

Unknown

Actions

Antagonist

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. Millward MJ, House C, Bowtell D, Webster L, Olver IN, Gore M, Copeman M, Lynch K, Yap A, Wang Y, Cohen PS, Zalcberg J: The multikinase inhibitor midostaurin (PKC412A) lacks activity in metastatic melanoma: a phase IIA clinical and biologic study. Br J Cancer. 2006 Oct 9;95(7):829-34. Epub 2006 Sep 12. [Article]

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Drug created at March 19, 2008 16:39 / Updated at February 20, 2024 23:54