Identification

Name
Ribociclib
Accession Number
DB11730
Type
Small Molecule
Groups
Approved, Investigational
Description

Ribociclib is a selective cyclin-dependent kinase inhibitor, a class of drugs that help slow the progression of cancer by inhibiting two proteins called cyclin-dependent kinase 4 and 6 (CDK4/6). These proteins, when over-activated, can enable cancer cells to grow and divide too quickly. Targeting CDK4/6 with enhanced precision may play a role in ensuring that cancer cells do not continue to replicate uncontrollably. Ribociclib was approved by the U.S. FDA in March, 2017 as Kisqali.

Structure
Thumb
Synonyms
  • Ribociclib
External IDs
LEE-011 / LEE-011A / LEE011 / LEE011A
Product Ingredients
IngredientUNIICASInChI Key
Ribociclib hydrochloride63YF7YKW7E1211443-80-9JZRSIQPIKASMEV-UHFFFAOYSA-N
Ribociclib succinateBG7HLX29191374639-75-4NHANOMFABJQAAH-UHFFFAOYSA-N
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
KisqaliTablet200 mgOralNovartisNot applicableNot applicableCanada
KisqaliTablet, film coated200 mg/1OralNovartis Pharmaceuticals Corporation2017-03-13Not applicableUs
KisqaliTablet, film coated200 mg/1OralNovartis Pharmaceuticals Corporation2017-03-13Not applicableUs
KisqaliTablet, film coated200 mg/1OralNovartis Pharmaceuticals Corporation2017-03-13Not applicableUs
Mixture Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing End
Kisqali Femara Co-packRibociclib (200 mg/1) + Letrozole (2.5 mg/1)KitNovartis Pharmaceuticals Corporation2017-05-04Not applicableUs
Kisqali Femara Co-packRibociclib (200 mg/1) + Letrozole (2.5 mg/1)KitNovartis Pharmaceuticals Corporation2017-05-04Not applicableUs
Kisqali Femara Co-packRibociclib (200 mg/1) + Letrozole (2.5 mg/1)KitNovartis Pharmaceuticals Corporation2017-05-04Not applicableUs
Categories
UNII
TK8ERE8P56
CAS number
1211441-98-3
Weight
Average: 434.548
Monoisotopic: 434.254257618
Chemical Formula
C23H30N8O
InChI Key
RHXHGRAEPCAFML-UHFFFAOYSA-N
InChI
InChI=1S/C23H30N8O/c1-29(2)22(32)19-13-16-14-26-23(28-21(16)31(19)17-5-3-4-6-17)27-20-8-7-18(15-25-20)30-11-9-24-10-12-30/h7-8,13-15,17,24H,3-6,9-12H2,1-2H3,(H,25,26,27,28)
IUPAC Name
7-cyclopentyl-N,N-dimethyl-2-{[5-(piperazin-1-yl)pyridin-2-yl]amino}-7H-pyrrolo[2,3-d]pyrimidine-6-carboxamide
SMILES
CN(C)C(=O)C1=CC2=CN=C(NC3=CC=C(C=N3)N3CCNCC3)N=C2N1C1CCCC1

Pharmacology

Indication

Kisqali (ribociclib) is a selective cyclin-dependent kinase inhibitor, a class of drugs that help slow the progression of cancer by inhibiting two proteins called cyclin-dependent kinase 4 and 6 (CDK4/6). These proteins, when over-activated, can enable cancer cells to grow and divide too quickly. Targeting CDK4/6 with enhanced precision may play a role in ensuring that cancer cells do not continue to replicate uncontrollably.

Associated Conditions
Pharmacodynamics
Not Available
Mechanism of action

Inhibition of cyclin-dependent kinase 4 and 6 (CDK4/6) may provide protection against oncogenic processes in specific tissue types. For example, CDK4 is not required for normal mammary tissue development based on knockout mouse studies, but it is needed for growth of Ras-induced mammary tumors, suggesting a potential therapeutic window for treatment with lower toxicity. Ribociclib was reported to be a most selective CDK4/6 inhibitor and to have dose dependent antitumor activity in a number of preclinical models. It inhibited growth of tumor cells by arresting the cells at the G1 checkpoint, which prevents the tumor cells from proliferating.

TargetActionsOrganism
ACyclin-dependent kinase 4
antagonist
inhibitor
Human
ACyclin-dependent kinase 6
antagonist
inhibitor
Human
Absorption

Ribociclib is orally bioavailable, highly selective inhibitor of CDK4/6 kinases with inhibitory IC50 concentrations in the low nanomolar range. Following oral dosing, ribociclib was rapidly absorbed with median Tmax ranging from 1 to 5 hours. Plasma concentrations increased approximately 2- to 3-fold from Cycle 1 Day 1 to Cycle 1 Day 18/21 due to accumulation, with steady state reached by approximately Day 8 on the basis of trough concentrations after repeated daily dosing. Dose-proportionality analyses demonstrated that exposure to ribociclib increased with dose, with both Cmax and area under the curve (AUC) increasing slightly more than proportional to dose, over the dose range 50–1,200 mg/day

Volume of distribution
Not Available
Protein binding
Not Available
Metabolism
Not Available
Route of elimination
Not Available
Half life

32.6 hours

Clearance
Not Available
Toxicity
Not Available
Affected organisms
  • Humans and other mammals
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
DrugInteraction
(R)-warfarinThe metabolism of (R)-warfarin can be decreased when combined with Ribociclib.
(S)-WarfarinThe metabolism of (S)-Warfarin can be decreased when combined with Ribociclib.
3,5-diiodothyropropionic acidThe metabolism of 3,5-diiodothyropropionic acid can be decreased when combined with Ribociclib.
4-hydroxycoumarinThe metabolism of 4-hydroxycoumarin can be decreased when combined with Ribociclib.
5-androstenedioneThe metabolism of 5-androstenedione can be decreased when combined with Ribociclib.
6-Deoxyerythronolide BThe metabolism of Ribociclib can be decreased when combined with 6-Deoxyerythronolide B.
6-O-benzylguanineThe metabolism of 6-O-benzylguanine can be decreased when combined with Ribociclib.
7-ethyl-10-hydroxycamptothecinThe metabolism of 7-ethyl-10-hydroxycamptothecin can be decreased when combined with Ribociclib.
9-aminocamptothecinThe metabolism of 9-aminocamptothecin can be decreased when combined with Ribociclib.
AbataceptThe metabolism of Ribociclib can be increased when combined with Abatacept.
Food Interactions
Not Available

References

General References
  1. Yu Q, Sicinska E, Geng Y, Ahnstrom M, Zagozdzon A, Kong Y, Gardner H, Kiyokawa H, Harris LN, Stal O, Sicinski P: Requirement for CDK4 kinase function in breast cancer. Cancer Cell. 2006 Jan;9(1):23-32. [PubMed:16413469]
  2. Rader J, Russell MR, Hart LS, Nakazawa MS, Belcastro LT, Martinez D, Li Y, Carpenter EL, Attiyeh EF, Diskin SJ, Kim S, Parasuraman S, Caponigro G, Schnepp RW, Wood AC, Pawel B, Cole KA, Maris JM: Dual CDK4/CDK6 inhibition induces cell-cycle arrest and senescence in neuroblastoma. Clin Cancer Res. 2013 Nov 15;19(22):6173-82. doi: 10.1158/1078-0432.CCR-13-1675. Epub 2013 Sep 17. [PubMed:24045179]
  3. Infante JR, Cassier PA, Gerecitano JF, Witteveen PO, Chugh R, Ribrag V, Chakraborty A, Matano A, Dobson JR, Crystal AS, Parasuraman S, Shapiro GI: A Phase I Study of the Cyclin-Dependent Kinase 4/6 Inhibitor Ribociclib (LEE011) in Patients with Advanced Solid Tumors and Lymphomas. Clin Cancer Res. 2016 Dec 1;22(23):5696-5705. Epub 2016 Aug 19. [PubMed:27542767]
  4. PDF Article- Ribociclib as First-Line Therapy for HR-Positive, Advanced Breast Cancer [Link]
  5. FDA approval [Link]
External Links
KEGG Drug
D10883
PubChem Compound
44631912
PubChem Substance
347828089
ChemSpider
30798107
BindingDB
148264
ChEMBL
CHEMBL3545110
PharmGKB
PA166153470
HET
6ZZ
Wikipedia
Ribociclib
AHFS Codes
  • 10:00.00 — Antineoplastic Agents
PDB Entries
5l2t

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
0RecruitingBasic ScienceSquamous Cell Carcinoma of the Head and Neck (SCCHN)1
0RecruitingTreatmentGlioblastoma Multiforme (GBM) / Meningiomas1
1Active Not RecruitingHealth Services ResearchAgnogenic Myeloid Metaplasia1
1Active Not RecruitingTreatmentBreast Cancer - Female / Breast Cancer - Male / Cancer, Breast1
1Active Not RecruitingTreatmentCancer, Breast2
1Active Not RecruitingTreatmentGlioblastomas / Gliomas1
1Active Not RecruitingTreatmentHormone Receptor Positive, HER2-negative, Advanced Breast Cancer1
1Active Not RecruitingTreatmentSquamous Cell Carcinoma of the Head and Neck (SCCHN)1
1CompletedOtherAdvanced or Metastatic Breast Cancer1
1CompletedTreatmentAdvanced Solid Tumors1
1CompletedTreatmentAdvanced Solid Tumors / Malignant Lymphomas1
1CompletedTreatmentImpaired Hepatic Function / Normal Hepatic Function1
1CompletedTreatmentImpaired Renal Function / Normal Renal Function1
1CompletedTreatmentLung Cancer Non-Small Cell Cancer (NSCLC)1
1CompletedTreatmentMalignant Rhabdoid Tumors (MRT), Neuroblastoma1
1Not Yet RecruitingTreatmentAcute Lymphoblastic Leukemia ALL1
1RecruitingDiagnosticMetastatic Breast Cancer (MBC) / Neoplasms, Breast / Rb+ Breast Cancer1
1RecruitingTreatmentAdvanced Breast Cancer1
1RecruitingTreatmentAdvanced Malignant Solid Neoplasm / Metastatic Malignant Solid Neoplasm1
1RecruitingTreatmentAdvanced or Metastatic ER+ Breast Cancer1
1RecruitingTreatmentAnaplastic Astrocytoma (AA) / Anaplastic Ependymoma / Anaplastic Ganglioglioma / Anaplastic Meningioma / Anaplastic Oligodendroglioma (AO) / Atypical Teratoid/Rhabdoid Tumor / Brain Cancer / Central Nervous System Neoplasms / Choroid Plexus Carcinoma / CNS Embryonal Tumor With Rhabdoid Features / CNS Tumors / Embryonal Tumor of CNS / Embryonal Tumor With Multilayered Rosettes (ETMR) / Embryonal Tumor, NOS / Ependymoma, NOS, WHO Grade II / Ependymoma, NOS, WHO Grade III / Ependymoma, Recurrent / Ependymoma, RELA Fusion Positive / Ependymomas / Ganglioneuroblastoma of Central Nervous System / Glioblastoma, IDH-mutant / Glioblastoma, IDH-wildtype / Glioblastomas / Glioma, Diffuse Midline, H3K27M-mutant / Glioma, High Grade / Glioma, Malignant / Glioma, Recurrent High Grade / Glioma, Recurrent Malignant / Gliomas / Medulloblastoma, Chromosome 9q Loss / Medulloblastoma, G3/G4 / Medulloblastoma, Group 3 / Medulloblastoma, Group 4 / Medulloblastoma, Non-WNT Non-SHH, NOS / Medulloblastoma, Non-WNT/Non-SHH / Medulloblastoma, PTCH1 Mutation / Medulloblastoma, SHH-activated and TP53 Mutant / Medulloblastoma, SHH-activated and TP53 Wildtype / Medulloblastoma, WNT-activated / Medulloblastoma; Unspecified Site / Medulloblastomas / Medulloepithelioma / Neoplasms / Neoplasms, Brain / Neoplasms, Neuroepithelial / Neuroblastoma. CNS / Neuroepithelial Tumor / Neuroepithelial Tumor, High Grade / Papillary Tumor of the Pineal Region (High-grade Only) / Pediatric Brain Tumor / Pineal Parenchymal Tumor of Intermediate Differentiation (High-grade Only) / Pinealoblastoma / Pleomorphic Xanthoastrocytoma, Anaplastic / Primitive Neuroectodermal Tumor / Recurrent Medulloblastoma / Refractory Brain Tumor1
1RecruitingTreatmentAnaplastic Astrocytoma (AA) / Bithalamic High Grade Glioma / Brain Stem Gliomas / Diffuse Intrinsic Pontine Glioma (DIPG) / Glioblastomas / High Grade Glioma (HGG) / Malignant Glioma of Brain1
1RecruitingTreatmentCancer of the Ovary / Fallopian Tube Cancer / Primary Peritoneal Cancer1
1RecruitingTreatmentCentral Nervous System Embryonal Tumor, Not Otherwise Specified / Malignant Gliomas / Recurrent Atypical Teratoid/Rhabdoid Tumor / Recurrent Childhood Ependymoma / Recurrent Diffuse Intrinsic Pontine Glioma / Recurrent Medulloblastoma / Refractory Diffuse Intrinsic Pontine Glioma1
1RecruitingTreatmentEGFR-mutant Non-small Cell Lung Cancer1
1RecruitingTreatmentHER2-Negative Breast Cancer / Metastatic Epithelial Ovarian Cancer / Metastatic Hormone-Receptor-Positive (HR+) Breast Cancer1
1RecruitingTreatmentMalignancies / Neuroblastomas1
1RecruitingTreatmentMetastatic Angiosarcoma / Metastatic Epithelioid Sarcoma / Metastatic Fibrosarcoma / Metastatic Leiomyosarcoma / Metastatic Liposarcoma / Metastatic Malignant Peripheral Nerve Sheath Tumor / Metastatic Synovial Sarcoma / Metastatic Undifferentiated Pleomorphic Sarcoma / Myxofibrosarcoma / Pleomorphic Rhabdomyosarcoma / Stage III Soft Tissue Sarcoma / Stage IV Soft Tissue Sarcoma / Undifferentiated (Embryonal) Sarcoma1
1TerminatedTreatmentMalignant Lymphomas / Solid Neoplasms1
1, 2Active Not RecruitingOtherSolid Tumors Harboring a BRAF V600 Mutation1
1, 2Active Not RecruitingTreatmentBithalamic High Grade Glioma / Diffuse Intrinsic Pontine Glioma (DIPG) / High Grade Glioma (HGG)1
1, 2Active Not RecruitingTreatmentCancer, Breast1
1, 2Active Not RecruitingTreatmentLiposarcoma1
1, 2CompletedTreatmentCancer, Breast1
1, 2CompletedTreatmentLocally Advanced or Metastatic NRAS Mutant Melanoma1
1, 2RecruitingTreatmentCancer, Breast1
1, 2RecruitingTreatmentChildren, Adolescents and Young Adults With Refractory or Recurrent Malignancies1
1, 2RecruitingTreatmentColorectal Cancers / Malignant Neoplasm of Pancreas / Tumors, Solid1
1, 2RecruitingTreatmentHormone-Resistant Prostate Cancer / Metastatic Hormone Refractory Prostate Cancer / Prostate Carcinoma Metastatic in the Bone / Stage IV Prostate Cancer1
1, 2RecruitingTreatmentPancreatic Adenocarcinoma Metastatic1
1, 2RecruitingTreatmentProstate Cancer1
1, 2RecruitingTreatmentTriple Negative Breast Cancer (TNBC)1
1, 2TerminatedTreatmentLocally Advanced Metastatic BRAF Mutant Melanoma / Locally Advanced or Metastatic BRAF Mutant Melanoma1
2Active Not RecruitingTreatmentCancer, Advanced / Cancers With a Mass, Bulky Tumor, Nodule, Lump, Advanced Cancer, Advanced Solid Tumors, Advanced Solid Malignancies / Continued Access to Study Treatment(s) / Continued Access to Study Treatment(s), Cancers With a Mass, Bulky Tumor, Nodule, Lump, Advanced Cancer, Advanced Solid Tumors, Advanced Solid Malignancies / Nodules / Tumors, Solid1
2Active Not RecruitingTreatmentCancer, Breast1
2Active Not RecruitingTreatmentEstrogen Receptor and/or Progesterone Receptor Positive / Estrogen Receptor Positive / HER2/Neu Negative / Progesterone Receptor Positive / Stage IV Breast Cancer AJCC v6 and v71
2Active Not RecruitingTreatmentEstrogen Receptor Positive / One to five years postmenopausal / RB1 Positive / Recurrent Fallopian Tube Carcinoma / Recurrent Ovarian Carcinoma / Recurrent Primary Peritoneal Carcinoma / Recurrent Uterine Corpus Carcinoma1
2Active Not RecruitingTreatmentGastrointestinal Cancers1
2Active Not RecruitingTreatmentLiposarcoma / Soft Tissue Sarcoma (STS)1
2Active Not RecruitingTreatmentMelanoma1
2CompletedTreatmentTeratoma1
2CompletedTreatmentTumors With CDK4/6 Pathway Activation1
2Not Yet RecruitingOtherHR+ HER2 Breast Cancer1
2Not Yet RecruitingTreatmentLow Grade Serous Carcinoma1
2RecruitingTreatmentBreast Cancer Metastatic1
2RecruitingTreatmentCancer, Breast4
2RecruitingTreatmentCarcinoma, Breast / Metastatic Breast Cancer (MBC)1
2RecruitingTreatmentEndometrial Carcinoma / Malignant Neoplasms of Female Genital Organs1
2RecruitingTreatmentHepatocellular,Carcinoma1
2RecruitingTreatmentLiposarcoma - Well Differentiated / Liposarcoma; Mixed Type / Liposarcomas, Dedifferentiated / Soft-Tissue Sarcoma1
2RecruitingTreatmentNeuroendocrine Tumors1
2RecruitingTreatmentSoft Tissue Sarcoma (STS)1
2TerminatedNot AvailableStage I Breast Carcinoma1
3Active Not RecruitingTreatmentAdvanced Breast Cancer / Antineoplastic Agents / Antineoplastic Agents, Hormonal / Breast Diseases / Estrogen Receptor Antagonists / Fulvestrant / Hormone Antagonists / Hormones, Hormone Substitutes, and Hormone Antagonists / Molecular Mechanisms of Pharmacological Action / Neoplasms / Neoplasms by Site / Neoplasms, Breast / Pharmacologic Actions / Therapeutic Uses1
3Active Not RecruitingTreatmentAdvanced Metastatic Breast Cancer / Advanced, Metastatic Breast Cancer1
3Active Not RecruitingTreatmentAdvanced, Metastatic Breast Cancer1
3Active Not RecruitingTreatmentCancer, Breast1
3Not Yet RecruitingTreatmentStage I Breast Carcinoma1
3RecruitingOtherCancer, Breast1
3RecruitingTreatmentAdvanced Metastatic Breast Cancer1
3RecruitingTreatmentCancer, Breast1
3RecruitingTreatmentCancer, Breast / HER 2 Negative Breast Cancer / Hormone Receptor Positive Tumor1
3WithdrawnTreatmentCancer, Breast1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage forms
FormRouteStrength
TabletOral200 mg
Tablet, film coatedOral200 mg/1
Kit
Prices
Not Available
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
US8685980No2014-04-012030-05-25Us
US9193732No2015-11-242031-11-09Us
US8415355No2013-04-092031-02-19Us
US8324225No2012-12-042028-06-17Us
US9416136No2016-08-162029-08-20Us
US8962630No2015-02-242029-12-09Us
US9868739No2018-01-162031-11-09Us

Properties

State
Not Available
Experimental Properties
Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.231 mg/mLALOGPS
logP2.5ALOGPS
logP2.38ChemAxon
logS-3.3ALOGPS
pKa (Strongest Acidic)11.59ChemAxon
pKa (Strongest Basic)8.87ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count7ChemAxon
Hydrogen Donor Count2ChemAxon
Polar Surface Area91.21 Å2ChemAxon
Rotatable Bond Count5ChemAxon
Refractivity125.59 m3·mol-1ChemAxon
Polarizability49.13 Å3ChemAxon
Number of Rings5ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleNoChemAxon
Predicted ADMET features
Not Available

Spectra

Mass Spec (NIST)
Not Available
Spectra
SpectrumSpectrum TypeSplash Key
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSNot Available

Taxonomy

Description
This compound belongs to the class of organic compounds known as pyridinylpiperazines. These are compounds containing a pyridinylpiperazine skeleton, which consists of a pyridine linked (not fused) to a piperazine by a bond by a single bond that is not part of a ring.
Kingdom
Organic compounds
Super Class
Organoheterocyclic compounds
Class
Diazinanes
Sub Class
Piperazines
Direct Parent
Pyridinylpiperazines
Alternative Parents
N-arylpiperazines / Pyrrolo[2,3-d]pyrimidines / Pyrimidinecarboxamides / 2-heteroaryl carboxamides / Pyrrole carboxamides / Dialkylarylamines / Aminopyridines and derivatives / Aminopyrimidines and derivatives / Substituted pyrroles / Imidolactams
show 8 more
Substituents
Pyridinylpiperazine / N-arylpiperazine / Pyrimidinecarboxamide / Pyrrolopyrimidine / Pyrrolo[2,3-d]pyrimidine / 2-heteroaryl carboxamide / Pyrrole-2-carboxamide / Pyrrole-2-carboxylic acid or derivatives / Tertiary aliphatic/aromatic amine / Dialkylarylamine
show 24 more
Molecular Framework
Aromatic heteropolycyclic compounds
External Descriptors
Not Available

Targets

Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Antagonist
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. Rader J, Russell MR, Hart LS, Nakazawa MS, Belcastro LT, Martinez D, Li Y, Carpenter EL, Attiyeh EF, Diskin SJ, Kim S, Parasuraman S, Caponigro G, Schnepp RW, Wood AC, Pawel B, Cole KA, Maris JM: Dual CDK4/CDK6 inhibition induces cell-cycle arrest and senescence in neuroblastoma. Clin Cancer Res. 2013 Nov 15;19(22):6173-82. doi: 10.1158/1078-0432.CCR-13-1675. Epub 2013 Sep 17. [PubMed:24045179]
Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Antagonist
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. Rader J, Russell MR, Hart LS, Nakazawa MS, Belcastro LT, Martinez D, Li Y, Carpenter EL, Attiyeh EF, Diskin SJ, Kim S, Parasuraman S, Caponigro G, Schnepp RW, Wood AC, Pawel B, Cole KA, Maris JM: Dual CDK4/CDK6 inhibition induces cell-cycle arrest and senescence in neuroblastoma. Clin Cancer Res. 2013 Nov 15;19(22):6173-82. doi: 10.1158/1078-0432.CCR-13-1675. Epub 2013 Sep 17. [PubMed:24045179]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
No
Actions
Substrate
Inhibitor
General Function
Vitamin d3 25-hydroxylase activity
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation react...
Gene Name
CYP3A4
Uniprot ID
P08684
Uniprot Name
Cytochrome P450 3A4
Molecular Weight
57342.67 Da
References
  1. Sorf A, Hofman J, Kucera R, Staud F, Ceckova M: Ribociclib shows potential for pharmacokinetic drug-drug interactions being a substrate of ABCB1 and potent inhibitor of ABCB1, ABCG2 and CYP450 isoforms in vitro. Biochem Pharmacol. 2018 Aug;154:10-17. doi: 10.1016/j.bcp.2018.04.013. Epub 2018 Apr 16. [PubMed:29673999]

Drug created on October 20, 2016 14:43 / Updated on December 16, 2018 06:59