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Identification
NamePonatinib
Accession NumberDB08901
TypeSmall Molecule
GroupsApproved
Description

Ponatinib is a novel Bcr-Abl tyrosine kinase inhibitor that is especially effective against the T315I mutation for the treatment of chronic myeloid leukemia. FDA approved on December 14, 2012.

Structure
Thumb
Synonyms
SynonymLanguageCode
AP 24534Not AvailableNot Available
AP24534Not AvailableNot Available
PonatinibumNot AvailableNot Available
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Iclusigtablet, film coated45 mgoralARIAD Pharmaceuticals, Inc.2012-12-14Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Iclusigtablet, film coated15 mgoralARIAD Pharmaceuticals, Inc.2012-12-14Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Generic Prescription ProductsNot Available
Over the Counter ProductsNot Available
International BrandsNot Available
Brand mixturesNot Available
Salts
Name/CASStructureProperties
Ponatinib Hydrochloride
Thumb
  • InChI Key: BWTNNZPNKQIADY-UHFFFAOYSA-N
  • Monoisotopic Mass: 568.19652187
  • Average Mass: 569.02
DBSALT000142
CategoriesNot Available
CAS number943319-70-8
WeightAverage: 532.5595
Monoisotopic: 532.219844131
Chemical FormulaC29H27F3N6O
InChI KeyPHXJVRSECIGDHY-UHFFFAOYSA-N
InChI
InChI=1S/C29H27F3N6O/c1-20-5-6-22(16-21(20)8-10-25-18-33-27-4-3-11-34-38(25)27)28(39)35-24-9-7-23(26(17-24)29(30,31)32)19-37-14-12-36(2)13-15-37/h3-7,9,11,16-18H,12-15,19H2,1-2H3,(H,35,39)
IUPAC Name
3-(2-{imidazo[1,2-b]pyridazin-3-yl}ethynyl)-4-methyl-N-{4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl}benzamide
SMILES
CN1CCN(CC2=CC=C(NC(=O)C3=CC(C#CC4=CN=C5C=CC=NN45)=C(C)C=C3)C=C2C(F)(F)F)CC1
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as n-phenylbenzamides. These are benzamides that are N-linked to a phenyl group via the carboxamide group.
KingdomOrganic compounds
Super ClassBenzenoids
ClassBenzene and substituted derivatives
Sub ClassBenzamides
Direct ParentN-phenylbenzamides
Alternative Parents
Substituents
  • N-phenylbenzamide
  • N-arylamide
  • Benzoic acid or derivatives
  • Phenylmethylamine
  • Benzylamine
  • Benzoyl
  • Aralkylamine
  • N-alkylpiperazine
  • N-methylpiperazine
  • Toluene
  • Pyridazine
  • Piperazine
  • N-substituted imidazole
  • 1,4-diazinane
  • Heteroaromatic compound
  • Imidazole
  • Azole
  • Tertiary aliphatic amine
  • Tertiary amine
  • Secondary carboxylic acid amide
  • Carboxamide group
  • Azacycle
  • Organoheterocyclic compound
  • Carboxylic acid derivative
  • Hydrocarbon derivative
  • Organooxygen compound
  • Organonitrogen compound
  • Organofluoride
  • Organohalogen compound
  • Carbonyl group
  • Amine
  • Alkyl halide
  • Alkyl fluoride
  • Aromatic heteropolycyclic compound
Molecular FrameworkAromatic heteropolycyclic compounds
External Descriptors
Pharmacology
IndicationPonatinib is indicated for the treatment of adult patients with chronic phase, accelerated phase, or blast phase chronic myeloid leukemia (CML) that is resistant or intolerant to prior tyrosine kinase inhibitor therapy or Philadelphia chromosome positive acute lymphoblastic leukemia (Ph+ALL) that is resistant or intolerant to prior tyrosine kinase inhibitor therapy.
PharmacodynamicsNot Available
Mechanism of actionPonatinib is a multi-target kinase inhibitor. Its primary cellular target is the Bcr-Abl tyrosine kinase protein which is constitutively active and promotes the progression of CML. This protein arises from the fused Bcr and Abl gene- what is commonly known as the Philadelphia chromosome. Ponatinib is unique in that it is especially useful in the treatment of resistant CML because it inhibits the tyrosine kinase activity of Abl and T315I mutant kinases. The T315I mutation confers resistance in cells as it prevents other Bcr-Abl inhibitors from binding to the Abl kinase. Other targets that ponatinib inhibits are members of the VEGFR, PDGFR, FGFR, EPH receptors and SRC families of kinases, and KIT, RET, TIE2, and FLT3. A decrease in tumour size expressing native or T315I mutant BCR-ABL have been observed in rats.
AbsorptionThe absolute bioavailability of ponatinib is unknown. Peak concentrations of ponatinib are observed within 6 hours after Iclusig oral administration. Food does not affect absorption of food. The aqueous solubility of ponatinib is pH dependent, with higher pH resulting in lower solubility. When 45 mg of ponatinib is given to cancer patients, the pharmacokinetic parameters are as follows: Cmax = 73 ng/mL; AUC = 1253 ng•hr/mL;
Volume of distribution

After oral administration of 45 mg ponatinib once daily for 28 days in cancer patients, the steady state volume of distribution is 1223 L. Ponatinib is a weak substrate for P-gp and ABCG2.

Protein binding> 99% bound to plasma proteins.
Metabolism

At least 64% of a ponatinib dose undergoes phase I and phase II metabolism. CYP3A4 and to a lesser extent CYP2C8, CYP2D6 and CYP3A5 are involved in the phase I metabolism of ponatinib in vitro. Ponatinib is also metabolized by esterases and/or amidases.

Route of eliminationPonatinib is mainly eliminated via feces. Following a single oral dose of [14C]-labeled ponatinib, approximately 87% of the radioactive dose is recovered in the feces and approximately 5% in the urine.
Half lifeAfter oral administration of 45 mg ponatinib once daily for 28 days in cancer patients, the terminal elimination half-life is 24 hours (range of 12 - 66 hours).
ClearanceNot Available
ToxicityThe most common non-hematologic adverse reactions (≥ 20%) were hypertension, rash, abdominal pain, fatigue, headache, dry skin, constipation, arthralgia, nausea, and pyrexia. Hematologic adverse reactions included thrombocytopenia, anemia, neutropenia, lymphopenia, and leukopenia.
Affected organisms
  • Humans and other mammals
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+1.0
Blood Brain Barrier+0.9444
Caco-2 permeable-0.5985
P-glycoprotein substrateSubstrate0.7205
P-glycoprotein inhibitor IInhibitor0.8197
P-glycoprotein inhibitor IIInhibitor0.9125
Renal organic cation transporterInhibitor0.5
CYP450 2C9 substrateNon-substrate0.8612
CYP450 2D6 substrateNon-substrate0.7047
CYP450 3A4 substrateSubstrate0.7636
CYP450 1A2 substrateNon-inhibitor0.8592
CYP450 2C9 substrateNon-inhibitor0.6804
CYP450 2D6 substrateNon-inhibitor0.764
CYP450 2C19 substrateInhibitor0.5563
CYP450 3A4 substrateNon-inhibitor0.5613
CYP450 inhibitory promiscuityHigh CYP Inhibitory Promiscuity0.6686
Ames testNon AMES toxic0.5331
CarcinogenicityNon-carcinogens0.8254
BiodegradationNot ready biodegradable1.0
Rat acute toxicity2.8377 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.8253
hERG inhibition (predictor II)Inhibitor0.7493
Pharmacoeconomics
ManufacturersNot Available
PackagersNot Available
Dosage forms
FormRouteStrength
Tablet, film coatedoral15 mg
Tablet, film coatedoral45 mg
PricesNot Available
Patents
CountryPatent NumberApprovedExpires (estimated)
United States81148742012-12-142026-12-22
Properties
StateSolid
Experimental Properties
PropertyValueSource
pKa2.77 and 7.8 FDA label
Predicted Properties
PropertyValueSource
Water Solubility0.00295 mg/mLALOGPS
logP3.94ALOGPS
logP4.97ChemAxon
logS-5.3ALOGPS
pKa (Strongest Acidic)11.36ChemAxon
pKa (Strongest Basic)8.03ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count5ChemAxon
Hydrogen Donor Count1ChemAxon
Polar Surface Area65.77 Å2ChemAxon
Rotatable Bond Count7ChemAxon
Refractivity152.63 m3·mol-1ChemAxon
Polarizability55.69 Å3ChemAxon
Number of Rings5ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
SpectraNot Available
References
Synthesis ReferenceNot Available
General Reference
  1. Reddy EP, Aggarwal AK: The ins and outs of bcr-abl inhibition. Genes Cancer. 2012 May;3(5-6):447-54. doi: 10.1177/1947601912462126. Pubmed
  2. FDA label
External Links
ATC CodesL01XE24
AHFS Codes
  • 10:00
PDB EntriesNot Available
FDA labelDownload (295 KB)
MSDSDownload (98 KB)
Interactions
Drug Interactions
Drug
AtazanavirCYP3A4 Inhibitors (Strong) may increase the serum concentration of PONATinib.
BoceprevirCYP3A4 Inhibitors (Strong) may increase the serum concentration of PONATinib.
CarbamazepineCYP3A4 Inducers (Strong) may decrease the serum concentration of PONATinib.
ClarithromycinCYP3A4 Inhibitors (Strong) may increase the serum concentration of PONATinib.
ClozapineMyelosuppressive Agents may enhance the adverse/toxic effect of CloZAPine. Specifically, the risk for agranulocytosis may be increased.
ConivaptanCYP3A4 Inhibitors (Strong) may increase the serum concentration of PONATinib.
DarunavirCYP3A4 Inhibitors (Strong) may increase the serum concentration of PONATinib.
DelavirdineCYP3A4 Inhibitors (Strong) may increase the serum concentration of PONATinib.
EnzalutamideCYP3A4 Inducers (Strong) may decrease the serum concentration of PONATinib.
FosamprenavirCYP3A4 Inhibitors (Strong) may increase the serum concentration of PONATinib.
FosphenytoinCYP3A4 Inducers (Strong) may decrease the serum concentration of PONATinib.
IndinavirCYP3A4 Inhibitors (Strong) may increase the serum concentration of PONATinib.
ItraconazoleCYP3A4 Inhibitors (Strong) may increase the serum concentration of PONATinib.
LopinavirCYP3A4 Inhibitors (Strong) may increase the serum concentration of PONATinib.
NefazodoneCYP3A4 Inhibitors (Strong) may increase the serum concentration of PONATinib.
NelfinavirCYP3A4 Inhibitors (Strong) may increase the serum concentration of PONATinib.
PhenobarbitalCYP3A4 Inducers (Strong) may decrease the serum concentration of PONATinib.
PhenytoinCYP3A4 Inducers (Strong) may decrease the serum concentration of PONATinib.
PosaconazoleCYP3A4 Inhibitors (Strong) may increase the serum concentration of PONATinib.
PrimidoneCYP3A4 Inducers (Strong) may decrease the serum concentration of PONATinib.
RifampicinCYP3A4 Inducers (Strong) may decrease the serum concentration of PONATinib.
RifapentineCYP3A4 Inducers (Strong) may decrease the serum concentration of PONATinib.
RitonavirCYP3A4 Inhibitors (Strong) may increase the serum concentration of PONATinib.
SaquinavirCYP3A4 Inhibitors (Strong) may increase the serum concentration of PONATinib.
TelaprevirCYP3A4 Inhibitors (Strong) may increase the serum concentration of PONATinib.
TelithromycinCYP3A4 Inhibitors (Strong) may increase the serum concentration of PONATinib.
VoriconazoleCYP3A4 Inhibitors (Strong) may increase the serum concentration of PONATinib.
Food InteractionsNot Available

Targets

1. Tyrosine-protein kinase ABL1

Kind: protein

Organism: Human

Pharmacological action: yes

Actions: inhibitor

Components

Name UniProt ID Details
Tyrosine-protein kinase ABL1 P00519 Details

References:

  1. FDA label
  2. Iqbal Z, Aleem A, Iqbal M, Naqvi MI, Gill A, Taj AS, Qayyum A, ur-Rehman N, Khalid AM, Shah IH, Khalid M, Haq R, Khan M, Baig SM, Jamil A, Abbas MN, Absar M, Mahmood A, Rasool M, Akhtar T: Sensitive detection of pre-existing BCR-ABL kinase domain mutations in CD34+ cells of newly diagnosed chronic-phase chronic myeloid leukemia patients is associated with imatinib resistance: implications in the post-imatinib era. PLoS One. 2013;8(2):e55717. doi: 10.1371/journal.pone.0055717. Epub 2013 Feb 8. Pubmed

2. Breakpoint cluster region protein

Kind: protein

Organism: Human

Pharmacological action: yes

Actions: inhibitor

Components

Name UniProt ID Details
Breakpoint cluster region protein P11274 Details

References:

  1. FDA label
  2. Iqbal Z, Aleem A, Iqbal M, Naqvi MI, Gill A, Taj AS, Qayyum A, ur-Rehman N, Khalid AM, Shah IH, Khalid M, Haq R, Khan M, Baig SM, Jamil A, Abbas MN, Absar M, Mahmood A, Rasool M, Akhtar T: Sensitive detection of pre-existing BCR-ABL kinase domain mutations in CD34+ cells of newly diagnosed chronic-phase chronic myeloid leukemia patients is associated with imatinib resistance: implications in the post-imatinib era. PLoS One. 2013;8(2):e55717. doi: 10.1371/journal.pone.0055717. Epub 2013 Feb 8. Pubmed

3. Mast/stem cell growth factor receptor Kit

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: inhibitor

Components

Name UniProt ID Details
Mast/stem cell growth factor receptor Kit P10721 Details

References:

  1. FDA label
  2. Gleixner KV, Peter B, Blatt K, Suppan V, Reiter A, Radia D, Hadzijusufovic E, Valent P: Synergistic growth-inhibitory effects of ponatinib and midostaurin (PKC412) on neoplastic mast cells carrying KIT D816V. Haematologica. 2013 Mar 28. Pubmed

4. Proto-oncogene tyrosine-protein kinase receptor Ret

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: inhibitor

Components

Name UniProt ID Details
Proto-oncogene tyrosine-protein kinase receptor Ret P07949 Details

References:

  1. FDA label
  2. De Falco V, Buonocore P, Muthu M, Torregrossa L, Basolo F, Billaud M, Gozgit JM, Carlomagno F, Santoro M: Ponatinib (AP24534) Is a Novel Potent Inhibitor of Oncogenic RET Mutants Associated With Thyroid Cancer. J Clin Endocrinol Metab. 2013 May;98(5):E811-9. doi: 10.1210/jc.2012-2672. Epub 2013 Mar 22. Pubmed

5. Angiopoietin-1 receptor

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: inhibitor

Components

Name UniProt ID Details
Angiopoietin-1 receptor Q02763 Details

References:

  1. FDA label

6. Receptor-type tyrosine-protein kinase FLT3

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: inhibitor

Components

Name UniProt ID Details
Receptor-type tyrosine-protein kinase FLT3 P36888 Details

References:

  1. FDA label
  2. Smith CC, Lasater EA, Zhu X, Lin KC, Stewart WK, Damon LE, Salerno S, Shah NP: Activity of ponatinib against clinically-relevant AC220-resistant kinase domain mutants of FLT3-ITD. Blood. 2013 Apr 18;121(16):3165-71. doi: 10.1182/blood-2012-07-442871. Epub 2013 Feb 21. Pubmed

7. Fibroblast growth factor receptor 1

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: inhibitor

Components

Name UniProt ID Details
Fibroblast growth factor receptor 1 P11362 Details

References:

  1. Ren M, Hong M, Liu G, Wang H, Patel V, Biddinger P, Silva J, Cowell J, Hao Z: Novel FGFR inhibitor ponatinib suppresses the growth of non-small cell lung cancer cells overexpressing FGFR1. Oncol Rep. 2013 Jun;29(6):2181-90. doi: 10.3892/or.2013.2386. Epub 2013 Apr 4. Pubmed
  2. Gozgit JM, Squillace RM, Wongchenko MJ, Miller D, Wardwell S, Mohemmad Q, Narasimhan NI, Wang F, Clackson T, Rivera VM: Combined targeting of FGFR2 and mTOR by ponatinib and ridaforolimus results in synergistic antitumor activity in FGFR2 mutant endometrial cancer models. Cancer Chemother Pharmacol. 2013 May;71(5):1315-23. doi: 10.1007/s00280-013-2131-z. Epub 2013 Mar 7. Pubmed

8. Fibroblast growth factor receptor 2

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: inhibitor

Components

Name UniProt ID Details
Fibroblast growth factor receptor 2 P21802 Details

References:

  1. Gozgit JM, Squillace RM, Wongchenko MJ, Miller D, Wardwell S, Mohemmad Q, Narasimhan NI, Wang F, Clackson T, Rivera VM: Combined targeting of FGFR2 and mTOR by ponatinib and ridaforolimus results in synergistic antitumor activity in FGFR2 mutant endometrial cancer models. Cancer Chemother Pharmacol. 2013 May;71(5):1315-23. doi: 10.1007/s00280-013-2131-z. Epub 2013 Mar 7. Pubmed

9. Fibroblast growth factor receptor 3

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: inhibitor

Components

Name UniProt ID Details
Fibroblast growth factor receptor 3 P22607 Details

References:

  1. Gozgit JM, Squillace RM, Wongchenko MJ, Miller D, Wardwell S, Mohemmad Q, Narasimhan NI, Wang F, Clackson T, Rivera VM: Combined targeting of FGFR2 and mTOR by ponatinib and ridaforolimus results in synergistic antitumor activity in FGFR2 mutant endometrial cancer models. Cancer Chemother Pharmacol. 2013 May;71(5):1315-23. doi: 10.1007/s00280-013-2131-z. Epub 2013 Mar 7. Pubmed

10. Fibroblast growth factor receptor 4

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: inhibitor

Components

Name UniProt ID Details
Fibroblast growth factor receptor 4 P22455 Details

References:

  1. Gozgit JM, Squillace RM, Wongchenko MJ, Miller D, Wardwell S, Mohemmad Q, Narasimhan NI, Wang F, Clackson T, Rivera VM: Combined targeting of FGFR2 and mTOR by ponatinib and ridaforolimus results in synergistic antitumor activity in FGFR2 mutant endometrial cancer models. Cancer Chemother Pharmacol. 2013 May;71(5):1315-23. doi: 10.1007/s00280-013-2131-z. Epub 2013 Mar 7. Pubmed

11. Tyrosine-protein kinase Lck

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: inhibitor

Components

Name UniProt ID Details
Tyrosine-protein kinase Lck P06239 Details

References:

  1. Gushwa NN, Kang S, Chen J, Taunton J: Selective targeting of distinct active site nucleophiles by irreversible SRC-family kinase inhibitors. J Am Chem Soc. 2012 Dec 19;134(50):20214-7. doi: 10.1021/ja310659j. Epub 2012 Dec 4. Pubmed

12. Proto-oncogene tyrosine-protein kinase Src

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: inhibitor

Components

Name UniProt ID Details
Proto-oncogene tyrosine-protein kinase Src P12931 Details

References:

  1. O’Hare T, Shakespeare WC, Zhu X, Eide CA, Rivera VM, Wang F, Adrian LT, Zhou T, Huang WS, Xu Q, Metcalf CA 3rd, Tyner JW, Loriaux MM, Corbin AS, Wardwell S, Ning Y, Keats JA, Wang Y, Sundaramoorthi R, Thomas M, Zhou D, Snodgrass J, Commodore L, Sawyer TK, Dalgarno DC, Deininger MW, Druker BJ, Clackson T: AP24534, a pan-BCR-ABL inhibitor for chronic myeloid leukemia, potently inhibits the T315I mutant and overcomes mutation-based resistance. Cancer Cell. 2009 Nov 6;16(5):401-12. doi: 10.1016/j.ccr.2009.09.028. Pubmed

13. Tyrosine-protein kinase Lyn

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: inhibitor

Components

Name UniProt ID Details
Tyrosine-protein kinase Lyn P07948 Details

References:

  1. O’Hare T, Shakespeare WC, Zhu X, Eide CA, Rivera VM, Wang F, Adrian LT, Zhou T, Huang WS, Xu Q, Metcalf CA 3rd, Tyner JW, Loriaux MM, Corbin AS, Wardwell S, Ning Y, Keats JA, Wang Y, Sundaramoorthi R, Thomas M, Zhou D, Snodgrass J, Commodore L, Sawyer TK, Dalgarno DC, Deininger MW, Druker BJ, Clackson T: AP24534, a pan-BCR-ABL inhibitor for chronic myeloid leukemia, potently inhibits the T315I mutant and overcomes mutation-based resistance. Cancer Cell. 2009 Nov 6;16(5):401-12. doi: 10.1016/j.ccr.2009.09.028. Pubmed

14. Vascular endothelial growth factor receptor 2

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: inhibitor

Components

Name UniProt ID Details
Vascular endothelial growth factor receptor 2 P35968 Details

References:

  1. O’Hare T, Shakespeare WC, Zhu X, Eide CA, Rivera VM, Wang F, Adrian LT, Zhou T, Huang WS, Xu Q, Metcalf CA 3rd, Tyner JW, Loriaux MM, Corbin AS, Wardwell S, Ning Y, Keats JA, Wang Y, Sundaramoorthi R, Thomas M, Zhou D, Snodgrass J, Commodore L, Sawyer TK, Dalgarno DC, Deininger MW, Druker BJ, Clackson T: AP24534, a pan-BCR-ABL inhibitor for chronic myeloid leukemia, potently inhibits the T315I mutant and overcomes mutation-based resistance. Cancer Cell. 2009 Nov 6;16(5):401-12. doi: 10.1016/j.ccr.2009.09.028. Pubmed

15. Platelet-derived growth factor receptor alpha

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: inhibitor

Components

Name UniProt ID Details
Platelet-derived growth factor receptor alpha P16234 Details

References:

  1. O’Hare T, Shakespeare WC, Zhu X, Eide CA, Rivera VM, Wang F, Adrian LT, Zhou T, Huang WS, Xu Q, Metcalf CA 3rd, Tyner JW, Loriaux MM, Corbin AS, Wardwell S, Ning Y, Keats JA, Wang Y, Sundaramoorthi R, Thomas M, Zhou D, Snodgrass J, Commodore L, Sawyer TK, Dalgarno DC, Deininger MW, Druker BJ, Clackson T: AP24534, a pan-BCR-ABL inhibitor for chronic myeloid leukemia, potently inhibits the T315I mutant and overcomes mutation-based resistance. Cancer Cell. 2009 Nov 6;16(5):401-12. doi: 10.1016/j.ccr.2009.09.028. Pubmed

Enzymes

1. Cytochrome P450 3A4

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: substrate

Components

Name UniProt ID Details
Cytochrome P450 3A4 P08684 Details

References:

  1. FDA label

2. Cytochrome P450 2C8

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: substrate inhibitor

Components

Name UniProt ID Details
Cytochrome P450 2C8 P10632 Details

References:

  1. FDA label

3. Cytochrome P450 2D6

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: substrate

Components

Name UniProt ID Details
Cytochrome P450 2D6 P10635 Details

References:

  1. FDA label

4. Cytochrome P450 3A5

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: substrate

Components

Name UniProt ID Details
Cytochrome P450 3A5 P20815 Details

References:

  1. FDA label

Transporters

1. Multidrug resistance protein 1

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: substrate inhibitor

Components

Name UniProt ID Details
Multidrug resistance protein 1 P08183 Details

References:

  1. FDA label

2. ATP-binding cassette sub-family G member 2

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: substrate inhibitor

Components

Name UniProt ID Details
ATP-binding cassette sub-family G member 2 Q9UNQ0 Details

References:

  1. FDA label

3. Bile salt export pump

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: inhibitor

Components

Name UniProt ID Details
Bile salt export pump O95342 Details

References:

  1. FDA label

Comments
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Drug created on June 08, 2013 16:03 / Updated on September 16, 2013 18:11