Trilaciclib

Identification

Summary

Trilaciclib is a CDK4 and CDK6 inhibitor to reduce the risk of chemotherapy induced myelosuppression.

Brand Names

Cosela

Generic Name

Trilaciclib

DrugBank Accession Number

DB15442

Background

Trilaciclib, or G1T28, is a CDK4 and CDK6 inhibitor, indicated to reduce the incidence of chemotherapy induced myelosuppression in patients before topotecan-containing or platinum and etoposide-containing chemotherapy for extensive stage small cell lung cancer.⁶ CDK4 and CDK6 inhibitors have been investigated since the mid 1990s for their use in tumorigenesis and chemotherapy.³ Trilaciclib was first described in the literature in 2016.¹

Trilaciclib was granted FDA approval on 12 February 2021.⁵

Type

Small Molecule

Groups

Approved, Investigational

Structure

3D

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MOLSDF3D-SDFPDBSMILESInChI

Similar Structures

Structure for Trilaciclib (DB15442)

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Weight

Average: 446.559
Monoisotopic: 446.254257618

Chemical Formula

C₂₄H₃₀N₈O

Synonyms

• Trilaciclib

External IDs

• G1T28

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Pharmacology

Indication

Trilaciclib is indicated to reduce the incidence of chemotherapy induced myelosuppression in patients prior to receiving platinum and etoposide-containing or topotecan-containing chemotherapy regimens for extensive-stage small cell lung cancer.⁶

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Associated Conditions

Indication Type	Indication	Combined Product Details	Approval Level	Age Group	Patient Characteristics	Dose Form
Prophylaxis of	Bone marrow suppression caused by chemotherapy		••••••••••••	•••••	•••••• ••••••••• •••••••• •••••• •••••••••••••• ••••••••••••	•••••••••
Prophylaxis of	Bone marrow suppression caused by chemotherapy		••••••••••••	•••••	•••••• ••••••••• ••••••••••••	•••••••••

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Contraindications & Blackbox Warnings

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Pharmacodynamics

Trilaciclib is indicated to reduce the incidence of chemotherapy induced myelosuppression in patients prior to receiving platinum and etoposide-containing or topotecan-containing chemotherapy regimens for extensive-stage small cell lung cancer.⁶ It has a short duration of action of approximately 16 hours, and a narrow therapeutic index.^1,6 Patients should be counselled regarding the risk of injection site reactions, hypersensitivity, and interstitial lung disease.⁶

Mechanism of action

Trilaciclib is inhibits cyclin-dependant kinase 4 (CDK4) at a concentration of 1 nmol/L and cyclin-dependent kinase 5 (CDK5) at 4 nmol/L.^1,6 Inhibition of CDK2, CDK5, and CDK7 is over 1000-fold less at these concentrations and inhibition of CDK9 is 50-fold less.¹

CDK4 and CDK5 are expressed in hematopoietic stem cells and progenitor cells.² They are capable of phosphorylating and inactivating the retinoblastoma protien; a tumor suppressor.^1,3 When trilaciclib is given to patients with retinoblastoma protein-null small cell lung cancer, it does not interfere with the intended chemotherapy induced cytotoxicity of cancer cells.¹ Inhibition of CDK4 and CDK5 leads to a reversible pause in the cell cycle in the G1 phase for approximately 16 hours.¹ The temporary cell cycle arrest prevents chemotherapy induced DNA damage in healthy cells, reducing the activity of caspases 3 and 7, which reduces apoptosis of healthy cells.¹

Other studies have shown inhibitors of CDK4 and CDK6 enhance T-cell activation, upregulating major histocompatibility complex (MHC) class I and II, and stabilize programmed death-ligand 1 (PD-L1).² Together these activities increase T-cell activity, increase antigen presentation, and sensitize cells to immune checkpoint inhibitors.²

Target	Actions	Organism
ACyclin-dependent kinase 4	inhibitor	Humans
ACyclin-dependent kinase 6	inhibitor	Humans
NCyclin-dependent kinase 9	inhibitor	Humans
NCyclin-dependent kinase 2	inhibitor	Humans
NCyclin-dependent kinase 5	inhibitor	Humans
NCyclin-dependent kinase 7	inhibitor	Humans

Absorption

C_max and AUC of trilaciclib increase proportionally with dose.^4,6

Volume of distribution

The volume of distribution of trilaciclib at steady state is 1130 L.⁶

Protein binding

Data regarding the protein binding of trilaciclib are not readily available.⁶

Metabolism

Data regarding the metabolism of trilaciclib are not readily available, however it is expected to be extensively metabolised.⁶

Route of elimination

79.1% of a radiolabelled dose is recovered in the feces, 7% as the unchanged parent compound.⁶ 14% of a radiolabelled dose is recovered in the urine, 2% as the unchanged parent compound.⁶

Half-life

The mean terminal half life of trilaciblib is approximately 14 h.⁶

Clearance

The clearance of trilaciclib is 158 L/h.⁶

Adverse Effects

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Toxicity

Data regarding overdoses of trilaciclib are not readily available.⁶ For grade 3 or worse injection site reactions, acute drug hypersensitivity reactions, and interstitial lung disease; or any other grade 4 toxicities; permanently discontinue trilacilib.⁶

Pathways

Not Available

Pharmacogenomic Effects/ADRs Browse all" title="About SNP Mediated Effects/ADRs" id="snp-actions-info" class="drug-info-popup" href="javascript:void(0);">

Not Available

Interactions

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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
Integrate drug-drug interactions in your software
Abemaciclib	The excretion of Abemaciclib can be decreased when combined with Trilaciclib.
Abrocitinib	The serum concentration of Trilaciclib can be increased when it is combined with Abrocitinib.
Acenocoumarol	The metabolism of Acenocoumarol can be increased when combined with Trilaciclib.
Acetaminophen	The metabolism of Acetaminophen can be increased when combined with Trilaciclib.
Acyclovir	The metabolism of Acyclovir can be increased when combined with Trilaciclib.

Food Interactions

No interactions found.

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Product Ingredients

Ingredient	UNII	CAS	InChI Key
Trilaciclib dihydrochloride	4BX07W725T	1977495-97-8	BRCYOXKEDFAUSA-UHFFFAOYSA-N

International/Other Brands

Cosela (G1 Therapeutics, Inc.)

Brand Name Prescription Products

Name	Dosage	Strength	Route	Labeller	Marketing Start	Marketing End	Region	Image
Cosela	Injection, powder, lyophilized, for solution	300 mg/20mL	Intravenous	G1 Therapeutics, Inc.	2021-02-12	Not applicable

Categories

ATC Codes

V03AF12 — Trilaciclib

• V03AF — Detoxifying agents for antineoplastic treatment
• V03A — ALL OTHER THERAPEUTIC PRODUCTS
• V03 — ALL OTHER THERAPEUTIC PRODUCTS
• V — VARIOUS

Drug Categories

• BCRP/ABCG2 Substrates
• Cyclin-dependent Kinase 4 Inhibitors
• Cyclin-dependent Kinase 6 Inhibitors
• Cyclin-Dependent Kinases, antagonists & inhibitors
• Cytochrome P-450 CYP1A2 Inducers
• Cytochrome P-450 CYP1A2 Inducers (strength unknown)
• Cytochrome P-450 CYP1A2 Inhibitors
• Cytochrome P-450 CYP1A2 Inhibitors (strength unknown)
• Cytochrome P-450 Enzyme Inducers
• Cytochrome P-450 Enzyme Inhibitors
• Detoxifying Agents for Antineoplastic Treatment
• Kinase Inhibitor
• MATE 1 Inhibitors
• MATE 2 Inhibitors
• MATE 2-K Inhibitors
• MATE inhibitors
• OCT2 Inhibitors
• P-glycoprotein substrates
• Protein Kinase Inhibitors

Classification

Not classified

Affected organisms

Not Available

Chemical Identifiers

UNII

U6072DO9XG

CAS number

1374743-00-6

InChI Key

PDGKHKMBHVFCMG-UHFFFAOYSA-N

InChI

InChI=1S/C24H30N8O/c1-30-9-11-31(12-10-30)18-5-6-20(25-15-18)28-23-26-14-17-13-19-22(33)27-16-24(7-3-2-4-8-24)32(19)21(17)29-23/h5-6,13-15H,2-4,7-12,16H2,1H3,(H,27,33)(H,25,26,28,29)

IUPAC Name

12'-{[5-(4-methylpiperazin-1-yl)pyridin-2-yl]amino}-2',5',11',13'-tetraazaspiro[cyclohexane-1,3'-tricyclo[7.4.0.0^{2,7}]tridecane]-1'(9'),7',10',12'-tetraen-6'-one

SMILES

CN1CCN(CC1)C1=CN=C(NC2=NC3=C(C=C4N3C3(CCCCC3)CNC4=O)C=N2)C=C1

References

General References

1. Bisi JE, Sorrentino JA, Roberts PJ, Tavares FX, Strum JC: Preclinical Characterization of G1T28: A Novel CDK4/6 Inhibitor for Reduction of Chemotherapy-Induced Myelosuppression. Mol Cancer Ther. 2016 May;15(5):783-93. doi: 10.1158/1535-7163.MCT-15-0775. Epub 2016 Jan 29. [Article]
2. Lai AY, Sorrentino JA, Dragnev KH, Weiss JM, Owonikoko TK, Rytlewski JA, Hood J, Yang Z, Malik RK, Strum JC, Roberts PJ: CDK4/6 inhibition enhances antitumor efficacy of chemotherapy and immune checkpoint inhibitor combinations in preclinical models and enhances T-cell activation in patients with SCLC receiving chemotherapy. J Immunother Cancer. 2020 Oct;8(2). pii: jitc-2020-000847. doi: 10.1136/jitc-2020-000847. [Article]
3. Peters G: The D-type cyclins and their role in tumorigenesis. J Cell Sci Suppl. 1994;18:89-96. doi: 10.1242/jcs.1994.supplement_18.13. [Article]
4. Tiessen RG, Roberts PJ, Sorrentino JA, White HS, Makhuli KM, Bisi JE, Strum JC, van Hoogdalem E, Malik RK: First-in-human Phase 1 safety, PK, and PD study of the CDK4/6 inhibitor G1T28. Journal of Clinical Oncology. 2015 May 20;33(15):2527-2527. [Article]
5. FDA News Release: FDA Approves Drug to Reduce Bone Marrow Suppression Caused by Chemotherapy [Link]
6. FDA Approved Drug Products: Cosela (Trilaciclib) Intravenous Injection [Link]

External Links

Human Metabolome Database

HMDB0304899

ChemSpider

58825997

BindingDB

253928

RxNav

2479690

ChEMBL

CHEMBL3894860

Wikipedia

CDK_inhibitor

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	Extensive-stage Small Cell Lung Cancer (SCLC)	1
4	Recruiting	Treatment	Extensive-stage Small Cell Lung Cancer (SCLC)	1
3	Active Not Recruiting	Treatment	Breast Cancer / Triple-Negative Breast Cancer	1
3	Completed	Treatment	Extensive-stage Small Cell Lung Cancer (SCLC)	1
3	Terminated	Treatment	Chemotherapeutic Agent Toxicity / Metastatic Colorectal Cancer (CRC) / Myelosuppression Adult	1

Pharmacoeconomics

Manufacturers

Not Available

Packagers

Not Available

Dosage Forms

Form	Route	Strength
Injection, powder, lyophilized, for solution	Intravenous	300 mg/20mL

Prices

Not Available

Patents

Patent Number	Pediatric Extension	Approved	Expires (estimated)	Region
US9487530	No	2016-11-08	2034-03-14
US10085992	No	2018-10-02	2034-03-14
US8598197	No	2013-12-03	2031-10-25
US8598186	No	2013-12-03	2031-10-25
US10927120	No	2021-02-23	2031-10-25
US9957276	No	2018-05-01	2031-10-25
US10189849	No	2019-01-29	2031-10-25
US10189850	No	2019-01-29	2031-10-25
US10966984	No	2021-04-06	2034-03-14
US11040042	No	2021-06-22	2034-03-14
US11529352	No	2019-07-23	2039-07-23
US11717523	No	2014-03-14	2034-03-14

Properties

State

Solid

Experimental Properties

Not Available

Predicted Properties

Property	Value	Source
Water Solubility	0.26 mg/mL	ALOGPS
logP	2.85	ALOGPS
logP	2.74	Chemaxon
logS	-3.2	ALOGPS
pKa (Strongest Acidic)	11.59	Chemaxon
pKa (Strongest Basic)	7.65	Chemaxon
Physiological Charge	1	Chemaxon
Hydrogen Acceptor Count	7	Chemaxon
Hydrogen Donor Count	2	Chemaxon
Polar Surface Area	91.21 Å2	Chemaxon
Rotatable Bond Count	3	Chemaxon
Refractivity	128.51 m3·mol-1	Chemaxon
Polarizability	50.52 Å3	Chemaxon
Number of Rings	6	Chemaxon
Bioavailability	1	Chemaxon
Rule of Five	Yes	Chemaxon
Ghose Filter	Yes	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	splash10-0002-0000900000-e063117a77803de07a58
Predicted MS/MS Spectrum - 10V, Negative (Annotated)	Predicted LC-MS/MS	splash10-0002-0001900000-63b0a558f87d6bf0176c
Predicted MS/MS Spectrum - 20V, Positive (Annotated)	Predicted LC-MS/MS	splash10-0f6t-0001900000-2f73e82a49249460ac92
Predicted MS/MS Spectrum - 20V, Negative (Annotated)	Predicted LC-MS/MS	splash10-00kb-0000900000-2504410fa4601f4a1e97
Predicted MS/MS Spectrum - 40V, Positive (Annotated)	Predicted LC-MS/MS	splash10-01oy-0009500000-8584c1c5c05a068189e2
Predicted MS/MS Spectrum - 40V, Negative (Annotated)	Predicted LC-MS/MS	splash10-00vm-0297700000-325a20f38c3700fa7530
Predicted 1H NMR Spectrum	1D NMR	Not Applicable
Predicted 13C NMR Spectrum	1D NMR	Not Applicable

Chromatographic Properties

Collision Cross Sections (CCS)

Not Available

Targets

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Details1. Cyclin-dependent kinase 4

Kind

Protein

Organism

Humans

Pharmacological action

Yes

Actions

Inhibitor

General Function

Cyclin-dependent protein serine/threonine kinase regulator activity

Specific Function

Ser/Thr-kinase component of cyclin D-CDK4 (DC) complexes that phosphorylate and inhibit members of the retinoblastoma (RB) protein family including RB1 and regulate the cell-cycle during G(1)/S tra...

Gene Name

CDK4

Uniprot ID

P11802

Uniprot Name

Cyclin-dependent kinase 4

Molecular Weight

33729.55 Da

References

1. Weiss JM, Csoszi T, Maglakelidze M, Hoyer RJ, Beck JT, Domine Gomez M, Lowczak A, Aljumaily R, Rocha Lima CM, Boccia RV, Hanna W, Nikolinakos P, Chiu VK, Owonikoko TK, Schuster SR, Hussein MA, Richards DA, Sawrycki P, Bulat I, Hamm JT, Hart LL, Adler S, Antal JM, Lai AY, Sorrentino JA, Yang Z, Malik RK, Morris SR, Roberts PJ, Dragnev KH: Myelopreservation with the CDK4/6 inhibitor trilaciclib in patients with small-cell lung cancer receiving first-line chemotherapy: a phase Ib/randomized phase II trial. Ann Oncol. 2019 Oct 1;30(10):1613-1621. doi: 10.1093/annonc/mdz278. [Article]
2. Daniel D, Kuchava V, Bondarenko I, Ivashchuk O, Reddy S, Jaal J, Kudaba I, Hart L, Matitashvili A, Pritchett Y, Morris SR, Sorrentino JA, Antal JM, Goldschmidt J: Trilaciclib prior to chemotherapy and atezolizumab in patients with newly diagnosed extensive-stage small cell lung cancer: A multicentre, randomised, double-blind, placebo-controlled Phase II trial. Int J Cancer. 2020 Dec 21. doi: 10.1002/ijc.33453. [Article]
3. Lai AY, Sorrentino JA, Dragnev KH, Weiss JM, Owonikoko TK, Rytlewski JA, Hood J, Yang Z, Malik RK, Strum JC, Roberts PJ: CDK4/6 inhibition enhances antitumor efficacy of chemotherapy and immune checkpoint inhibitor combinations in preclinical models and enhances T-cell activation in patients with SCLC receiving chemotherapy. J Immunother Cancer. 2020 Oct;8(2). pii: jitc-2020-000847. doi: 10.1136/jitc-2020-000847. [Article]
4. Li C, Hart L, Owonikoko TK, Aljumaily R, Rocha Lima CM, Conkling PR, Webb RT, Jotte RM, Schuster S, Edenfield WJ, Smith DA, Sale M, Roberts PJ, Malik RK, Sorrentino JA: Trilaciclib dose selection: an integrated pharmacokinetic and pharmacodynamic analysis of preclinical data and Phase Ib/IIa studies in patients with extensive-stage small cell lung cancer. Cancer Chemother Pharmacol. 2021 Feb 17. pii: 10.1007/s00280-021-04239-9. doi: 10.1007/s00280-021-04239-9. [Article]
5. Hart LL, Ferrarotto R, Andric ZG, Beck JT, Subramanian J, Radosavljevic DZ, Zaric B, Hanna WT, Aljumaily R, Owonikoko TK, Verhoeven D, Xiao J, Morris SR, Antal JM, Hussein MA: Myelopreservation with Trilaciclib in Patients Receiving Topotecan for Small Cell Lung Cancer: Results from a Randomized, Double-Blind, Placebo-Controlled Phase II Study. Adv Ther. 2021 Jan;38(1):350-365. doi: 10.1007/s12325-020-01538-0. Epub 2020 Oct 29. [Article]
6. FDA Approved Drug Products: Cosela (Trilaciclib) Intravenous Injection [Link]

Details2. Cyclin-dependent kinase 6

Kind

Protein

Organism

Humans

Pharmacological action

Yes

Actions

Inhibitor

General Function

Cyclin-dependent protein serine/threonine kinase activity

Specific Function

Serine/threonine-protein kinase involved in the control of the cell cycle and differentiation; promotes G1/S transition. Phosphorylates pRB/RB1 and NPM1. Interacts with D-type G1 cyclins during int...

Gene Name

CDK6

Uniprot ID

Q00534

Uniprot Name

Cyclin-dependent kinase 6

Molecular Weight

36938.025 Da

References

1. Weiss JM, Csoszi T, Maglakelidze M, Hoyer RJ, Beck JT, Domine Gomez M, Lowczak A, Aljumaily R, Rocha Lima CM, Boccia RV, Hanna W, Nikolinakos P, Chiu VK, Owonikoko TK, Schuster SR, Hussein MA, Richards DA, Sawrycki P, Bulat I, Hamm JT, Hart LL, Adler S, Antal JM, Lai AY, Sorrentino JA, Yang Z, Malik RK, Morris SR, Roberts PJ, Dragnev KH: Myelopreservation with the CDK4/6 inhibitor trilaciclib in patients with small-cell lung cancer receiving first-line chemotherapy: a phase Ib/randomized phase II trial. Ann Oncol. 2019 Oct 1;30(10):1613-1621. doi: 10.1093/annonc/mdz278. [Article]
2. Daniel D, Kuchava V, Bondarenko I, Ivashchuk O, Reddy S, Jaal J, Kudaba I, Hart L, Matitashvili A, Pritchett Y, Morris SR, Sorrentino JA, Antal JM, Goldschmidt J: Trilaciclib prior to chemotherapy and atezolizumab in patients with newly diagnosed extensive-stage small cell lung cancer: A multicentre, randomised, double-blind, placebo-controlled Phase II trial. Int J Cancer. 2020 Dec 21. doi: 10.1002/ijc.33453. [Article]
3. Lai AY, Sorrentino JA, Dragnev KH, Weiss JM, Owonikoko TK, Rytlewski JA, Hood J, Yang Z, Malik RK, Strum JC, Roberts PJ: CDK4/6 inhibition enhances antitumor efficacy of chemotherapy and immune checkpoint inhibitor combinations in preclinical models and enhances T-cell activation in patients with SCLC receiving chemotherapy. J Immunother Cancer. 2020 Oct;8(2). pii: jitc-2020-000847. doi: 10.1136/jitc-2020-000847. [Article]
4. Li C, Hart L, Owonikoko TK, Aljumaily R, Rocha Lima CM, Conkling PR, Webb RT, Jotte RM, Schuster S, Edenfield WJ, Smith DA, Sale M, Roberts PJ, Malik RK, Sorrentino JA: Trilaciclib dose selection: an integrated pharmacokinetic and pharmacodynamic analysis of preclinical data and Phase Ib/IIa studies in patients with extensive-stage small cell lung cancer. Cancer Chemother Pharmacol. 2021 Feb 17. pii: 10.1007/s00280-021-04239-9. doi: 10.1007/s00280-021-04239-9. [Article]
5. Hart LL, Ferrarotto R, Andric ZG, Beck JT, Subramanian J, Radosavljevic DZ, Zaric B, Hanna WT, Aljumaily R, Owonikoko TK, Verhoeven D, Xiao J, Morris SR, Antal JM, Hussein MA: Myelopreservation with Trilaciclib in Patients Receiving Topotecan for Small Cell Lung Cancer: Results from a Randomized, Double-Blind, Placebo-Controlled Phase II Study. Adv Ther. 2021 Jan;38(1):350-365. doi: 10.1007/s12325-020-01538-0. Epub 2020 Oct 29. [Article]
6. FDA Approved Drug Products: Cosela (Trilaciclib) Intravenous Injection [Link]

Details3. Cyclin-dependent kinase 9

Kind

Protein

Organism

Humans

Pharmacological action

No

Actions

Inhibitor

Curator comments

Inhibition is 50-fold less than inhibition of CDK4

General Function

Transcription regulatory region dna binding

Specific Function

Protein kinase involved in the regulation of transcription. Member of the cyclin-dependent kinase pair (CDK9/cyclin-T) complex, also called positive transcription elongation factor b (P-TEFb), whic...

Gene Name

CDK9

Uniprot ID

P50750

Uniprot Name

Cyclin-dependent kinase 9

Molecular Weight

42777.155 Da

References

1. Bisi JE, Sorrentino JA, Roberts PJ, Tavares FX, Strum JC: Preclinical Characterization of G1T28: A Novel CDK4/6 Inhibitor for Reduction of Chemotherapy-Induced Myelosuppression. Mol Cancer Ther. 2016 May;15(5):783-93. doi: 10.1158/1535-7163.MCT-15-0775. Epub 2016 Jan 29. [Article]

Details4. Cyclin-dependent kinase 2

Kind

Protein

Organism

Humans

Pharmacological action

No

Actions

Inhibitor

Curator comments

Inhibition is 1000-fold less than inhibition of CDK4

General Function

Metal ion binding

Specific Function

Serine/threonine-protein kinase involved in the control of the cell cycle; essential for meiosis, but dispensable for mitosis. Phosphorylates CTNNB1, USP37, p53/TP53, NPM1, CDK7, RB1, BRCA2, MYC, N...

Gene Name

CDK2

Uniprot ID

P24941

Uniprot Name

Cyclin-dependent kinase 2

Molecular Weight

33929.215 Da

References

1. Bisi JE, Sorrentino JA, Roberts PJ, Tavares FX, Strum JC: Preclinical Characterization of G1T28: A Novel CDK4/6 Inhibitor for Reduction of Chemotherapy-Induced Myelosuppression. Mol Cancer Ther. 2016 May;15(5):783-93. doi: 10.1158/1535-7163.MCT-15-0775. Epub 2016 Jan 29. [Article]

Details5. Cyclin-dependent kinase 5

Kind

Protein

Organism

Humans

Pharmacological action

No

Actions

Inhibitor

Curator comments

Inhibition is 1000-fold less than inhibition of CDK4

General Function

Tau-protein kinase activity

Specific Function

Proline-directed serine/threonine-protein kinase essential for neuronal cell cycle arrest and differentiation and may be involved in apoptotic cell death in neuronal diseases by triggering abortive...

Gene Name

CDK5

Uniprot ID

Q00535

Uniprot Name

Cyclin-dependent-like kinase 5

Molecular Weight

33304.125 Da

References

1. Bisi JE, Sorrentino JA, Roberts PJ, Tavares FX, Strum JC: Preclinical Characterization of G1T28: A Novel CDK4/6 Inhibitor for Reduction of Chemotherapy-Induced Myelosuppression. Mol Cancer Ther. 2016 May;15(5):783-93. doi: 10.1158/1535-7163.MCT-15-0775. Epub 2016 Jan 29. [Article]

Details6. Cyclin-dependent kinase 7

Kind

Protein

Organism

Humans

Pharmacological action

No

Actions

Inhibitor

Curator comments

Inhibition is 1000-fold less than inhibition of CDK4

General Function

Transcription coactivator activity

Specific Function

Serine/threonine kinase involved in cell cycle control and in RNA polymerase II-mediated RNA transcription. Cyclin-dependent kinases (CDKs) are activated by the binding to a cyclin and mediate the ...

Gene Name

CDK7

Uniprot ID

P50613

Uniprot Name

Cyclin-dependent kinase 7

Molecular Weight

39038.005 Da

References

1. Bisi JE, Sorrentino JA, Roberts PJ, Tavares FX, Strum JC: Preclinical Characterization of G1T28: A Novel CDK4/6 Inhibitor for Reduction of Chemotherapy-Induced Myelosuppression. Mol Cancer Ther. 2016 May;15(5):783-93. doi: 10.1158/1535-7163.MCT-15-0775. Epub 2016 Jan 29. [Article]

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Drug created at May 20, 2019 15:32 / Updated at February 21, 2024 02:33