Glasdegib

Identification

Summary

Glasdegib is a sonic hedgehog receptor inhibitor used to treat newly diagnosed acute myeloid leukemia in patients over 75 years who cannot receive intense chemotherapy.

Brand Names
Daurismo
Generic Name
Glasdegib
DrugBank Accession Number
DB11978
Background

Glasdegib, also known as PF-04449913, is a small-molecule hedgehog signaling inhibitor selected under the group of benzimidazoles. In early research, benzimidazoles attracted large interest as they represented a class of inhibitors with low molecular weight, potent inhibitory activity, and lacking unstable functionality.1 The great lipophilicity of this group of compounds brought interest to further modification. This analysis concluded that the presence of p-cyano ureas presented good physicochemical and pharmacokinetic properties from which glasdegib was developed.1

Glasdegib was developed by Pfizer Inc and approved on November 21, 2018 by the FDA for the treatment of Acute Myeloid Leukemia (AML).11 Glasdegib targets cancerous cells by inhibiting the sonic hedgehog receptor smoothened (SMO), a transmembrane protein involved in the Hedgehog (Hh) signaling cascade.5 Aberrant of Hh signaling is one of the main pathophysiologies of AML, with observed overexpression or constitutive activation of SMO.6,7 Although the efficacy of glasdegib monotherapy is limited, the landmark Phase 2 Bright AML 1003 trial showed a superior overall survival and complete response when glasdegib is combined with low dose cytarabine. Currently, the current gold standard of AML in older patients is still venetoclax with hypomethylation agents, new clinical combinations of glasdegib are being tested in hope of replacing venetoclax due to glasdegib's more favorable side effects profile.5

Type
Small Molecule
Groups
Approved, Investigational
Structure
Weight
Average: 374.448
Monoisotopic: 374.185509352
Chemical Formula
C21H22N6O
Synonyms
  • Glasdegib
External IDs
  • PF 04449913
  • PF-04449913
  • PF-4449913

Pharmacology

Indication

Glasdegib, in combination with cytarabine, is indicated for the treatment of newly diagnosed acute myeloid leukemia in adult patients who are over 75 years old or that have co-morbidities that preclude intensive induction chemotherapy.9

Acute myeloid leukemia is characterized by abnormal production of myeloblasts, red cells, or platelets. It is considered a cancer of blood and bone marrow and it is the most common type of acute leukemia in adults.10

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Associated Conditions
Indication TypeIndicationCombined Product DetailsApproval LevelAge GroupPatient CharacteristicsDose Form
Used in combination to treatAcute myeloid leukemiaRegimen in combination with: Cytarabine (DB00987)•••••••••••••••••• •••••••••••••• •••• ••••••
Used in combination to treatAcute myeloid leukemia (aml)Regimen in combination with: Cytarabine (DB00987)•••••••••••••••••••••••••••••• •••• •••••••• ••••••••• ••••••••••••••••••
Contraindications & Blackbox Warnings
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Pharmacodynamics

In preclinical studies, glasdegib achieved a significant reduction in leukemic stem cell burden in xenograft models and a reduction in cell population expressing leukemic stem cell markers.2

In clinical trials, glasdegib demonstrated a marked downregulation of more than 80% of the expression of glioma-associated transcriptional regulator GL11 in skin. In this same study 8% of the studied individuals with acute myeloid leukemia achieved morphological complete remission while 31% achieved stable disease state.2

The latest clinical trial proved glasdegib to generate an overall survival of 8.3 months which was almost double to what has been observed in patients under low-dose cytarabine treatment. As well, there have been reports of dose-dependent QTc prolongation in patients administered with glasdegib.9

Mechanism of action

Glasdegib is a potent and selective inhibitor of the hedgehog signaling pathway that acts by binding to the smoothened (SMO) receptor.1

The hedgehog signaling pathway is involved in maintenance of neural and skin stem cells. In this pathway, the binding of specific ligands to the transmembrane receptor patched (PTCH1) allows the activation of the transcriptional regulators GL11, GL12 and modulation of the gene expression through SMO-mediated signaling. The aberrant activation of the hedgehog pathway is thought to be implicated in the pathogenesis of chronic myeloid leukemia, medulloblastoma and basal cell carcinoma due to the hyperproliferative state that a modification on this pathway will produce.3

TargetActionsOrganism
ASmoothened homolog
inhibitor
Humans
Absorption

Glasdegib presents a dose-proportional pharmacokinetic profile which is observed by the presence of a broad dose-proportional maximum plasma concentration. In this study and on a dose of 50 mg, the median time to reach a maximum concentration of 321 ng/ml was of 4 hours with an AUC of 9587 ng.h/ml.2 The oral bioavailability of glasdegib is reported to be of 55%.1

In a multiple dose study of 50 mg, the Cmax, tmax and AUC was reported to be 542 ng/ml, 4 h and 9310 ng.h/ml respectively. In this same study, the average concentration at a steady state was of 388 ng/ml.2

The absorption rates of glasdegib can be modified by the concomitant consumption of a high-fat, high-calorie meal.Label

Volume of distribution

Glasdegib reported volume of distribution in a dose of 50 mg is 225 L.2 The geometric mean (%CV) apparent volume of distribution (Vz/F) was 188 L (20%) in patients with hematologic malignancies.12

Protein binding

Glasdegib is reported to be 91% protein bounded which is explained due to its high lipophilic profile.8

Metabolism

After oral administration, glasdegib was primarily metabolized by CYP3A4 with minor contributions of CYP2C8 and UGT1A9. The amount of unchanged glasdegib in plasma accounts only for 69% of the administered dose.4

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Route of elimination

From a single oral dose of 100 mg radiolabeled glasdegib, 49% is eliminated in the urine from which 17% is excreted as the unchanged form while 42% is eliminated in feces where 20% represents the unchanged form.4,12

Half-life

The reported half-life of glasdegib is of 17.4 hours.8

Clearance

The clearance rate of 50 mg of glasdegib is reported to be of 5.22 L/h.2 The geometric mean (%CV) apparent clearance of 6.45 L/h (25%) following 100 mg once daily dosing in patients with hematologic malignancies.12

Adverse Effects
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Toxicity

Based on its mechanism of action and findings in animal embryo-fetal developmental toxicity studies, glasdegib can cause fetal harm when administered to a pregnant woman. There are no clinical data on the use of glasdegib in pregnant women to inform of a drug-associated risk of major birth defects and miscarriage. Glasdegib is not recommended for use during pregnancy. Conduct pregnancy testing in female patients of reproductive potential prior to initiating treatment with glasdegib. Report pregnancy exposures to Pfizer at 1-800-438-1985.12

In animal embryo-fetal developmental toxicity studies, repeat-dose oral administration of glasdegib during organogenesis at maternal exposures that were less than the human exposure at the recommended dose resulted in embryotoxicity, fetotoxicity, and teratogenicity in rats and rabbits. Advise pregnant women of the potential risk to a fetus.12

Carcinogenicity studies have not been performed with glasdegib. Glasdegib was not mutagenic in vitro in the bacterial reverse mutation (Ames) assay and was not clastogenic in the in vitro chromosome aberration assay in human lymphocytes. Glasdegib was not clastogenic or aneugenic in the rat micronucleus assay.12

Based on nonclinical safety findings, glasdegib has the potential to impair reproductive function in males. Men should seek advice on effective fertility preservation before treatment. In repeat-dose toxicity studies in rats, findings observed in the male reproductive tract included adverse testicular changes with glasdegib at doses ≥50 mg/kg/day and consisted of minimal to severe hypospermatogenesis characterized by partial to complete loss of spermatogonia, spermatocytes and spermatids and testicular degeneration. Hypospermatogenesis did not recover whereas testicular degeneration did recover. The dose at which testicular effects were observed in male rats was identified as 50 mg/kg/day with corresponding systemic exposures that were approximately 6.6 times (based on AUC) those associated with the observed human exposure at the 100 mg once daily dose.

There is no specific antidote for DAURISMO. Management of DAURISMO overdose should include symptomatic treatment and ECG monitoring. Glasdegib has been administered in clinical studies up to a dose of 640 mg/day. At the highest dosage, the adverse reactions that were dose-limiting were nausea, vomiting, dehydration, hypotension, fatigue, and dizziness.12

Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
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.
DrugInteraction
AbametapirThe serum concentration of Glasdegib can be increased when it is combined with Abametapir.
AbataceptThe metabolism of Glasdegib can be increased when combined with Abatacept.
AbemaciclibThe serum concentration of Abemaciclib can be increased when it is combined with Glasdegib.
AbirateroneThe metabolism of Glasdegib can be decreased when combined with Abiraterone.
AbrocitinibThe serum concentration of Glasdegib can be increased when it is combined with Abrocitinib.
Food Interactions
  • Avoid St. John's Wort. This herb induces CYP3A metabolism and may reduce serum levels of glasdegib.
  • Take at the same time every day.
  • Take with or without food.

Products

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Product Ingredients
IngredientUNIICASInChI Key
Glasdegib hydrochloride4Y7R3PBO4V1095173-64-0OCHAAZGYSAHXOF-LJLRIERRSA-N
Glasdegib maleateTH2EV99S4Z2030410-25-2VJCVKWFBWAVYOC-UIXXXISESA-N
Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
DaurismoTablet, film coated100 mgOralPfizer Europe Ma Eeig2021-03-16Not applicableEU flag
DaurismoTablet, film coated25 mgOralPfizer Europe Ma Eeig2021-03-16Not applicableEU flag
DaurismoTablet, film coated100 mg/1OralPfizer Laboratories Div Pfizer Inc2018-12-10Not applicableUS flag
DaurismoTablet, film coated100 mgOralPfizer Europe Ma Eeig2021-03-16Not applicableEU flag
DaurismoTablet100 mgOralPfizer Canada Ulc2020-08-10Not applicableCanada flag

Categories

ATC Codes
L01XJ03 — Glasdegib
Drug Categories
Chemical TaxonomyProvided by Classyfire
Description
This compound belongs to the class of organic compounds known as n-phenylureas. These are compounds containing a N-phenylurea moiety, which is structurally characterized by a phenyl group linked to one nitrogen atom of a urea group.
Kingdom
Organic compounds
Super Class
Benzenoids
Class
Benzene and substituted derivatives
Sub Class
N-phenylureas
Direct Parent
N-phenylureas
Alternative Parents
Benzimidazoles / Benzonitriles / Aralkylamines / Piperidines / Imidazoles / Heteroaromatic compounds / Ureas / Trialkylamines / Nitriles / Azacyclic compounds
show 3 more
Substituents
Amine / Aralkylamine / Aromatic heteropolycyclic compound / Azacycle / Azole / Benzimidazole / Benzonitrile / Carbonitrile / Carbonyl group / Cyanide
show 15 more
Molecular Framework
Aromatic heteropolycyclic compounds
External Descriptors
Not Available
Affected organisms
  • Humans and other mammals

Chemical Identifiers

UNII
K673DMO5H9
CAS number
1095173-27-5
InChI Key
SFNSLLSYNZWZQG-VQIMIIECSA-N
InChI
InChI=1S/C21H22N6O/c1-27-11-10-16(24-21(28)23-15-8-6-14(13-22)7-9-15)12-19(27)20-25-17-4-2-3-5-18(17)26-20/h2-9,16,19H,10-12H2,1H3,(H,25,26)(H2,23,24,28)/t16-,19-/m1/s1
IUPAC Name
1-[(2R,4R)-2-(1H-1,3-benzodiazol-2-yl)-1-methylpiperidin-4-yl]-3-(4-cyanophenyl)urea
SMILES
CN1CC[C@H](C[C@@H]1C1=NC2=CC=CC=C2N1)NC(=O)NC1=CC=C(C=C1)C#N

References

Synthesis Reference

Munchhof MJ, Li Q, Shavnya A, et al. Discovery of PF-04449913, a Potent and Orally Bioavailable Inhibitor of Smoothened. ACS Med Chem Lett. 2012;3(2):106-11.

General References
  1. Munchhof MJ, Li Q, Shavnya A, Borzillo GV, Boyden TL, Jones CS, LaGreca SD, Martinez-Alsina L, Patel N, Pelletier K, Reiter LA, Robbins MD, Tkalcevic GT: Discovery of PF-04449913, a Potent and Orally Bioavailable Inhibitor of Smoothened. ACS Med Chem Lett. 2011 Dec 21;3(2):106-11. doi: 10.1021/ml2002423. eCollection 2012 Feb 9. [Article]
  2. Minami Y, Minami H, Miyamoto T, Yoshimoto G, Kobayashi Y, Munakata W, Onishi Y, Kobayashi M, Ikuta M, Chan G, Woolfson A, Ono C, Shaik MN, Fujii Y, Zheng X, Naoe T: Phase I study of glasdegib (PF-04449913), an oral smoothened inhibitor, in Japanese patients with select hematologic malignancies. Cancer Sci. 2017 Aug;108(8):1628-1633. doi: 10.1111/cas.13285. Epub 2017 Jun 19. [Article]
  3. Irvine DA, Copland M: Targeting hedgehog in hematologic malignancy. Blood. 2012 Mar 8;119(10):2196-204. doi: 10.1182/blood-2011-10-383752. Epub 2012 Jan 5. [Article]
  4. Lam JL, Vaz A, Hee B, Liang Y, Yang X, Shaik MN: Metabolism, excretion and pharmacokinetics of [(14)C]glasdegib (PF-04449913) in healthy volunteers following oral administration. Xenobiotica. 2017 Dec;47(12):1064-1076. doi: 10.1080/00498254.2016.1261307. Epub 2017 Jan 3. [Article]
  5. Iyer SG, Stanchina M, Bradley TJ, Watts J: Profile of Glasdegib for the Treatment of Newly Diagnosed Acute Myeloid Leukemia (AML): Evidence to Date. Cancer Manag Res. 2022 Aug 1;14:2267-2272. doi: 10.2147/CMAR.S195723. eCollection 2022. [Article]
  6. Jamieson C, Martinelli G, Papayannidis C, Cortes JE: Hedgehog Pathway Inhibitors: A New Therapeutic Class for the Treatment of Acute Myeloid Leukemia. Blood Cancer Discov. 2020 Aug 11;1(2):134-145. doi: 10.1158/2643-3230.BCD-20-0007. eCollection 2020 Sep. [Article]
  7. Terao T, Minami Y: Targeting Hedgehog (Hh) Pathway for the Acute Myeloid Leukemia Treatment. Cells. 2019 Apr 3;8(4):312. doi: 10.3390/cells8040312. [Article]
  8. Bethesda (2006). Drugs and Lactation Database. National Library of Medicine.
  9. FDA news [Link]
  10. NIH [Link]
  11. FDA Approved Drug Products: Daurismo (glasdegib) oral tablets [Link]
  12. FDA Approved Drug Products: Daurismo (glasdegib) oral tablets (March 2023) [Link]
  13. EMA Assessment Report: Daurismo International non-proprietary name glasdegib [Link]
  14. Pfizer Glasdegib product information [File]
PubChem Compound
25166913
PubChem Substance
347828300
ChemSpider
28518072
BindingDB
50385635
RxNav
2105845
ChEBI
145428
ChEMBL
CHEMBL2043437
ZINC
ZINC000068251434
Wikipedia
Glasdegib
FDA label
Download (572 KB)
MSDS
Download (24.6 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
3Active Not RecruitingHealth Services ResearchSoft Tissue Sarcoma1
3CompletedTreatmentAcute Myeloid Leukemia1
3CompletedTreatmentAcute Myeloid Leukemia / Chronic Myelomonocytic Leukemia / Myelodysplastic Syndrome1
3RecruitingTreatmentAcute Myeloid Leukemia1
3TerminatedTreatmentAcute Myeloid Leukemia1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage Forms
FormRouteStrength
TabletOral100 mg
TabletOral25 mg
Tablet, film coatedOral100 mg/1
Tablet, film coatedOral100 MG
Tablet, film coatedOral25 mg/1
Tablet, film coatedOral25 MG
Prices
Not Available
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)Region
US8431597No2013-04-302028-06-29US flag
US8148401No2012-04-032031-01-30US flag
US10414748No2019-09-172036-04-13US flag
US11168066No2021-11-092036-04-13US flag

Properties

State
Solid
Experimental Properties
PropertyValueSource
water solubility0.02 mg/ml (in the form of di-HCl monohydrate salt)Munchhof M., et al. (2011). ACS Med Chem Lett.
logP2.28Munchhof M., et al. (2011). ACS Med Chem Lett.
Caco2 permeability0.00000598Munchhof M., et al. (2011). ACS Med Chem Lett.
pKa6Munchhof M., et al. (2011). ACS Med Chem Lett.
Predicted Properties
PropertyValueSource
Water Solubility0.0469 mg/mLALOGPS
logP2.68ALOGPS
logP2.28Chemaxon
logS-3.9ALOGPS
pKa (Strongest Acidic)11.39Chemaxon
pKa (Strongest Basic)6.67Chemaxon
Physiological Charge0Chemaxon
Hydrogen Acceptor Count4Chemaxon
Hydrogen Donor Count3Chemaxon
Polar Surface Area96.84 Å2Chemaxon
Rotatable Bond Count3Chemaxon
Refractivity108.26 m3·mol-1Chemaxon
Polarizability40.73 Å3Chemaxon
Number of Rings4Chemaxon
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/MSsplash10-004i-0049000000-95adfc803c1d43ca30ba
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSsplash10-004i-0395000000-e2bf38ac0737cad4bda1
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSsplash10-004i-0189000000-56dfc6f45f475567ee71
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSsplash10-002f-9581000000-f9bde29ab07cf8da4667
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSsplash10-05ox-4938000000-f6d5c9edfc7d0b28d876
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSsplash10-014i-2922000000-38b506603028dba063be
Predicted 1H NMR Spectrum1D NMRNot Applicable
Predicted 13C NMR Spectrum1D NMRNot Applicable
Chromatographic Properties
Collision Cross Sections (CCS)
AdductCCS Value (Å2)Source typeSource
[M-H]-179.29291
predicted
DeepCCS 1.0 (2019)
[M+H]+181.68848
predicted
DeepCCS 1.0 (2019)
[M+Na]+188.2357
predicted
DeepCCS 1.0 (2019)

Targets

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insights and accelerate drug research.
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Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Inhibitor
General Function
Wnt-protein binding
Specific Function
G protein-coupled receptor that probably associates with the patched protein (PTCH) to transduce the hedgehog's proteins signal. Binding of sonic hedgehog (SHH) to its receptor patched is thought t...
Gene Name
SMO
Uniprot ID
Q99835
Uniprot Name
Smoothened homolog
Molecular Weight
86395.95 Da
References
  1. Munchhof MJ, Li Q, Shavnya A, Borzillo GV, Boyden TL, Jones CS, LaGreca SD, Martinez-Alsina L, Patel N, Pelletier K, Reiter LA, Robbins MD, Tkalcevic GT: Discovery of PF-04449913, a Potent and Orally Bioavailable Inhibitor of Smoothened. ACS Med Chem Lett. 2011 Dec 21;3(2):106-11. doi: 10.1021/ml2002423. eCollection 2012 Feb 9. [Article]

Enzymes

Kind
Protein
Organism
Humans
Pharmacological action
No
Actions
Substrate
General Function
Steroid 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 oxidizes a variety of structurally un...
Gene Name
CYP2C8
Uniprot ID
P10632
Uniprot Name
Cytochrome P450 2C8
Molecular Weight
55824.275 Da
References
  1. Lam JL, Vaz A, Hee B, Liang Y, Yang X, Shaik MN: Metabolism, excretion and pharmacokinetics of [(14)C]glasdegib (PF-04449913) in healthy volunteers following oral administration. Xenobiotica. 2017 Dec;47(12):1064-1076. doi: 10.1080/00498254.2016.1261307. Epub 2017 Jan 3. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
No
Actions
Substrate
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. FDA Approved Drug Products: Daurismo (glasdegib) oral tablets (March 2023) [Link]
Kind
Protein
Organism
Humans
Pharmacological action
No
Actions
Substrate
General Function
Retinoic acid binding
Specific Function
UDPGT is of major importance in the conjugation and subsequent elimination of potentially toxic xenobiotics and endogenous compounds. This isoform has specificity for phenols. Isoform 2 lacks trans...
Gene Name
UGT1A9
Uniprot ID
O60656
Uniprot Name
UDP-glucuronosyltransferase 1-9
Molecular Weight
59940.495 Da
References
  1. Lam JL, Vaz A, Hee B, Liang Y, Yang X, Shaik MN: Metabolism, excretion and pharmacokinetics of [(14)C]glasdegib (PF-04449913) in healthy volunteers following oral administration. Xenobiotica. 2017 Dec;47(12):1064-1076. doi: 10.1080/00498254.2016.1261307. Epub 2017 Jan 3. [Article]

Carriers

Kind
Protein
Organism
Humans
Pharmacological action
No
Actions
Binder
General Function
Toxic substance binding
Specific Function
Serum albumin, the main protein of plasma, has a good binding capacity for water, Ca(2+), Na(+), K(+), fatty acids, hormones, bilirubin and drugs. Its main function is the regulation of the colloid...
Gene Name
ALB
Uniprot ID
P02768
Uniprot Name
Serum albumin
Molecular Weight
69365.94 Da
References
  1. EMA Assessment Report: Daurismo International non-proprietary name glasdegib [Link]
Kind
Protein group
Organism
Humans
Pharmacological action
No
Actions
Binder
General Function
Not Available
Specific Function
Functions as transport protein in the blood stream. Binds various ligands in the interior of its beta-barrel domain. Also binds synthetic drugs and influences their distribution and availability in...

Components:
References
  1. EMA Assessment Report: Daurismo International non-proprietary name glasdegib [Link]

Transporters

Kind
Protein
Organism
Humans
Pharmacological action
No
Actions
Substrate
Inhibitor
General Function
Xenobiotic-transporting atpase activity
Specific Function
Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells.
Gene Name
ABCB1
Uniprot ID
P08183
Uniprot Name
Multidrug resistance protein 1
Molecular Weight
141477.255 Da
References
  1. FDA Approved Drug Products: Daurismo (glasdegib) oral tablets (March 2023) [Link]
Kind
Protein
Organism
Humans
Pharmacological action
No
Actions
Substrate
Inhibitor
General Function
Xenobiotic-transporting atpase activity
Specific Function
High-capacity urate exporter functioning in both renal and extrarenal urate excretion. Plays a role in porphyrin homeostasis as it is able to mediates the export of protoporhyrin IX (PPIX) both fro...
Gene Name
ABCG2
Uniprot ID
Q9UNQ0
Uniprot Name
ATP-binding cassette sub-family G member 2
Molecular Weight
72313.47 Da
References
  1. FDA Approved Drug Products: Daurismo (glasdegib) oral tablets (March 2023) [Link]
Kind
Protein
Organism
Humans
Pharmacological action
No
Actions
Inhibitor
General Function
Monovalent cation:proton antiporter activity
Specific Function
Solute transporter for tetraethylammonium (TEA), 1-methyl-4-phenylpyridinium (MPP), cimetidine, N-methylnicotinamide (NMN), metformin, creatinine, guanidine, procainamide, topotecan, estrone sulfat...
Gene Name
SLC47A1
Uniprot ID
Q96FL8
Uniprot Name
Multidrug and toxin extrusion protein 1
Molecular Weight
61921.585 Da
References
  1. FDA Approved Drug Products: Daurismo (glasdegib) oral tablets (March 2023) [Link]
Kind
Protein
Organism
Humans
Pharmacological action
No
Actions
Inhibitor
General Function
Drug transmembrane transporter activity
Specific Function
Solute transporter for tetraethylammonium (TEA), 1-methyl-4-phenylpyridinium (MPP), cimetidine, N-methylnicotinamide, metformin, creatinine, guanidine, procainamide, topotecan, estrone sulfate, acy...
Gene Name
SLC47A2
Uniprot ID
Q86VL8
Uniprot Name
Multidrug and toxin extrusion protein 2
Molecular Weight
65083.915 Da
References
  1. FDA Approved Drug Products: Daurismo (glasdegib) oral tablets (March 2023) [Link]

Drug created at October 20, 2016 21:07 / Updated at March 19, 2024 11:06