Vismodegib

Identification

Summary

Vismodegib is a hedgehog pathway inhibitor used to treat patients with locally advanced or metastatic basal cell carcinoma.

Brand Names
Erivedge
Generic Name
Vismodegib
DrugBank Accession Number
DB08828
Background

Vismodegib is an orally active small molecule that inhibits the hedgehog signaling pathway by binding to and inhibiting the transmembrane protein smoothened homologue (SMO).4,5,6 It was discovered by high-throughput screening of a library of small-molecule compounds and subsequent optimization through medicinal chemistry.1 Since it targets the hedgehog signaling pathway, vismodegib has anti-tumor activity in basal-cell carcinoma. The Hedgehog signaling pathway plays an important role in the development of organs and tissues during embryogenesis. Afterwards, it is silenced in all cells and tissues, except for hair, skin and stem cells. However, dysregulated or aberrant Hedgehog signaling has been associated with basal cell carcinoma pathogenesis.3,6 In January 2012, vismodegib was approved by the FDA for the treatment of adult basal cell carcinoma. In July 2013, it was approved by the EMA, and since then, it has been approved by several other countries.2,5,6

Type
Small Molecule
Groups
Approved, Investigational
Structure
Weight
Average: 421.297
Monoisotopic: 420.010218428
Chemical Formula
C19H14Cl2N2O3S
Synonyms
  • 2-chloro-N-(4-chloro-3-pyridin-2-yl)phenyl)-4-(methylsulfonyl)benzamide
  • Benzamide, 2-chloro-N-(4-chloro-3-(2-pyridinyl)phenyl)-4-(methylsulfonyl)-
  • Vismodegib
  • Vismodégib
  • Vismodegibum
External IDs
  • GDC-0449
  • NSC-747691
  • NSC-755986
  • RG-3616

Pharmacology

Indication

Vismodegib is indicated for the treatment of adults with metastatic basal cell carcinoma, or with locally advanced basal cell carcinoma that has recurred following surgery or who are not candidates for surgery and who are not candidates for radiation.6

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Associated Conditions
Indication TypeIndicationCombined Product DetailsApproval LevelAge GroupPatient CharacteristicsDose Form
Treatment ofLocally advanced basal cell carcinoma•••••••••••••••••••• • ••••••••• ••• •••••••• ••••••• •• ••••••••••••••••
Treatment ofLocally advanced basal cell carcinoma••••••••••••••••••••••••••• ••••••••• ••••••••••••••
Treatment ofMetastatic basal cell carcinoma••••••••••••••••••••••••
Contraindications & Blackbox Warnings
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Pharmacodynamics

Vismodegib selectively binds to and inhibits the transmembrane protein smoothened homologue (SMO) to inhibit the Hedgehog signalling pathway. Following 7 days of 150 mg once-daily dosing, the use of vismodegib was not associated with a clinically significant QT interval prolongation.6 Vismodegib can cause embryo-fetal death or severe birth defects, as well as severe cutaneous adverse reactions and musculoskeletal adverse reactions. In pediatric patients given vismodegib, premature fusion of the epiphyses has been reported.6

Mechanism of action

During embryogenesis, the Hedgehog signaling pathway plays an important role in cell growth, differentiation apoptosis and self-renewal. After this developmental stage, the Hedgehog signaling pathway is silenced in all cells and tissues, except for hair, skin and stem cells. Mutations on elements of the Hedgehog signaling pathway may result in uncontrolled proliferation of basal skin cells, and dysregulated or aberrant Hedgehog signaling has been associated with the pathogenesis of basal cell carcinoma. Therefore, drugs that target and block this pathway, such as vismodegib, may be used to treat this condition. Vismodegib binds to and inhibits the transmembrane protein smoothened homologue (SMO), a protein that leads to the activation and nuclear translocation of several factors involved in the Hedgehog signaling pathway, inhibiting the activation of downstream Hedgehog target genes.3,6

TargetActionsOrganism
ASmoothened homolog
antagonist
inhibitor
Humans
Absorption

Vismodegib appears to have a nonlinear pharmacokinetic profile following daily oral dosing, and steady state is achieved within 7 days. A dose increase from 150 mg to 540 mg (1 to 3.6 times the recommended dose) does not lead to an increase in steady-state plasma concentrations. With a once-daily dose of 150 mg, the average plasma concentration of vismodegib at steady state is approximately 23 µM. The absolute bioavailability of a single dose of vismodegib is 31.8%. Absorption is saturable and is not affected by food.6

Volume of distribution

The volume of distribution of vismodegib ranges between 16.4 and 26.6 L.6

Protein binding

Vismodegib has high plasma protein binding (>99%). Vismodegib binds to plasma albumin and alpha-1-acid glycoprotein (saturable binding).6

Metabolism

Vismodegib is mainly metabolized by CYP2C9 and CYP3A4 in the liver; however, more than 98% of total systemic vismodegib is not metabolized. Metabolic pathways of vismodegib in humans include oxidation, glucuronidation, and pyridine ring cleavage. The two most abundant oxidative metabolites recovered in feces are produced in vitro by recombinant CYP2C9 and CYP3A4/5.6

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Route of elimination

Vismodegib is excreted mostly unchanged. Vismodegib and its metabolites are mainly eliminated through feces. Approximately 82% and 4.4% of the administered dose are recovered in feces and urine, respectively.6

Half-life

The half-life of vismodegib after a single dose is 12 days, and after continuous daily dosing is 4 days.6

Clearance

Not Available

Adverse Effects
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Toxicity

Toxicity information regarding vismodegib is not readily available. Patients experiencing an overdose are at an increased risk of severe adverse effects such as severe cutaneous adverse reactions and musculoskeletal adverse reactions. Symptomatic and supportive measures are recommended. Patients treated with vismodegib have an increased risk of embryo-fetal death and significant birth defects. Common adverse event include muscle spasms, alopecia, dysgeusia, weight loss, fatigue, nausea, diarrhea, decreased appetite, constipation, arthralgias, vomiting, and ageusia.6

Based on the results of in vitro and in vivo studies, vismodegib is not mutagenic. No evidence of carcinogenicity was found in mice and rats given vismodegib. A 26-week rat fertility study found that at doses of 100 mg/kg/day, vismodegib has no effects on male reproductive organs or fertility. In female rats, the administration of vismodegib was associated with decreased implantations, increased percent preimplantation loss, and decreased numbers of dams with viable embryos.6

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
AbemaciclibVismodegib may decrease the excretion rate of Abemaciclib which could result in a higher serum level.
AfatinibVismodegib may decrease the excretion rate of Afatinib which could result in a higher serum level.
AllopurinolVismodegib may decrease the excretion rate of Allopurinol which could result in a higher serum level.
AlpelisibThe serum concentration of Alpelisib can be increased when it is combined with Vismodegib.
AmbroxolThe risk or severity of methemoglobinemia can be increased when Vismodegib is combined with Ambroxol.
Food Interactions
  • Take with or without food. Food does not affect absorption. The Cmax and AUC of vismodegib at steady state are not affected by food.

Products

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International/Other Brands
Erivedge (Genentech)
Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
ErivedgeCapsule150 mgOralHoffmann La Roche2013-08-09Not applicableCanada flag
ErivedgeCapsule150 mg/1OralGenentech, Inc.2012-01-30Not applicableUS flag
ErivedgeCapsule150 mgOralRoche Registration Gmb H2020-12-22Not applicableEU flag

Categories

ATC Codes
L01XJ01 — Vismodegib
Drug Categories
Chemical TaxonomyProvided by Classyfire
Description
This compound belongs to the class of organic compounds known as benzanilides. These are aromatic compounds containing an anilide group in which the carboxamide group is substituted with a benzene ring. They have the general structure RNC(=O)R', where R,R'= benzene.
Kingdom
Organic compounds
Super Class
Benzenoids
Class
Benzene and substituted derivatives
Sub Class
Anilides
Direct Parent
Benzanilides
Alternative Parents
Phenylpyridines / 2-halobenzoic acids and derivatives / Benzamides / Benzenesulfonyl compounds / Benzoyl derivatives / Chlorobenzenes / Aryl chlorides / Vinylogous halides / Sulfones / Heteroaromatic compounds
show 8 more
Substituents
2-halobenzoic acid or derivatives / 2-phenylpyridine / Aromatic heteromonocyclic compound / Aryl chloride / Aryl halide / Azacycle / Benzamide / Benzanilide / Benzenesulfonyl group / Benzoic acid or derivatives
show 23 more
Molecular Framework
Aromatic heteromonocyclic compounds
External Descriptors
sulfone, benzamides, pyridines, monochlorobenzenes (CHEBI:66903)
Affected organisms
  • Humans and other mammals

Chemical Identifiers

UNII
25X868M3DS
CAS number
879085-55-9
InChI Key
BPQMGSKTAYIVFO-UHFFFAOYSA-N
InChI
InChI=1S/C19H14Cl2N2O3S/c1-27(25,26)13-6-7-14(17(21)11-13)19(24)23-12-5-8-16(20)15(10-12)18-4-2-3-9-22-18/h2-11H,1H3,(H,23,24)
IUPAC Name
2-chloro-N-[4-chloro-3-(pyridin-2-yl)phenyl]-4-methanesulfonylbenzamide
SMILES
CS(=O)(=O)C1=CC(Cl)=C(C=C1)C(=O)NC1=CC=C(Cl)C(=C1)C1=CC=CC=N1

References

Synthesis Reference

Gunzner-Toste, JL., et al. (2020). Pyridyl inhibitors of hedgehog signalling (U.S. Patent No. 2020/0010420 A1 ). U.S. Patent and Trademark Office. https://patentimages.storage.googleapis.com/72/c1/79/c08582c18507d5/US20200010420A1.pdf

General References
  1. Von Hoff DD, LoRusso PM, Rudin CM, Reddy JC, Yauch RL, Tibes R, Weiss GJ, Borad MJ, Hann CL, Brahmer JR, Mackey HM, Lum BL, Darbonne WC, Marsters JC Jr, de Sauvage FJ, Low JA: Inhibition of the hedgehog pathway in advanced basal-cell carcinoma. N Engl J Med. 2009 Sep 17;361(12):1164-72. doi: 10.1056/NEJMoa0905360. Epub 2009 Sep 2. [Article]
  2. Sandhiya S, Melvin G, Kumar SS, Dkhar SA: The dawn of hedgehog inhibitors: Vismodegib. J Pharmacol Pharmacother. 2013 Jan;4(1):4-7. doi: 10.4103/0976-500X.107628. [Article]
  3. Aditya S, Rattan A: Vismodegib: A smoothened inhibitor for the treatment of advanced basal cell carcinoma. Indian Dermatol Online J. 2013 Oct;4(4):365-8. doi: 10.4103/2229-5178.120685. [Article]
  4. Abou-Alfa GK, Lewis LD, LoRusso P, Maitland M, Chandra P, Cheeti S, Colburn D, Williams S, Simmons B, Graham RA: Pharmacokinetics and safety of vismodegib in patients with advanced solid malignancies and hepatic impairment. Cancer Chemother Pharmacol. 2017 Jul;80(1):29-36. doi: 10.1007/s00280-017-3315-8. Epub 2017 May 18. [Article]
  5. Dessinioti C, Plaka M, Stratigos AJ: Vismodegib for the treatment of basal cell carcinoma: results and implications of the ERIVANCE BCC trial. Future Oncol. 2014 May;10(6):927-36. doi: 10.2217/fon.14.50. [Article]
  6. FDA Approved Drug Products: ERIVEDGE (vismodegib) capsules for oral use (March 2023) [Link]
  7. MedChemExpress: Vismodegib SDS [Link]
Human Metabolome Database
HMDB0259838
KEGG Drug
D09992
PubChem Compound
24776445
PubChem Substance
175427109
ChemSpider
23337846
BindingDB
50249522
RxNav
1242987
ChEBI
66903
ChEMBL
CHEMBL473417
ZINC
ZINC000040899447
PharmGKB
PA166048558
PDBe Ligand
VIS
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Vismodegib
PDB Entries
5l7i / 8hje

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
4CompletedTreatmentBasal Cell Carcinoma (BCC)1
4CompletedTreatmentLocally Advanced Basal Cell Carcinoma / Metastatic Basal cell carcinoma1
2Active Not RecruitingScreeningAdvanced Malignant Solid Tumor / Bladder Carcinoma / Breast Carcinoma / Carcinoma of the Head and Neck / Carcinoma of the Skin / Cervical Carcinoma / Colon Carcinoma / Colorectal Carcinoma (CRC) / Endometrial Carcinoma / Esophageal Carcinoma / Gastric Carcinoma / Glioma / Liver and Intrahepatic Bile Duct Carcinoma / Lung Carcinoma / Lymphoma / Malignant Uterine Neoplasm / Melanoma / Multiple Myeloma (MM) / Ovarian Carcinoma / Pancreatic Carcinoma / Prostate Carcinoma / Rectal Carcinoma / Recurrent Bladder Carcinoma / Recurrent Breast Carcinoma / Recurrent Cervical Carcinoma / Recurrent Colon Carcinoma / Recurrent Colorectal Carcinoma / Recurrent Esophageal Carcinoma / Recurrent Gastric Carcinoma / Recurrent Gliomas / Recurrent Head and Neck Carcinoma / Recurrent Liver Carcinoma / Recurrent Lung Carcinoma / Recurrent Lymphoma / Recurrent Malignant Solid Neoplasm / Recurrent Melanoma / Recurrent multiple myeloma / Recurrent Ovarian Carcinoma / Recurrent Pancreatic Carcinoma / Recurrent Prostate Carcinoma / Recurrent Rectal Carcinoma / Recurrent Skin Carcinoma / Recurrent Thyroid Gland Carcinoma / Recurrent Uterine Corpus Cancer / Refractory Lymphomas / Refractory Malignant Solid Neoplasm / Refractory Multiple Myeloma / Renal Carcinoma / Thyroid Gland Carcinoma / Uterine Corpus Cancer1
2Active Not RecruitingTreatmentBreast Cancer / Gastrointestinal Tract Cancer / Non-Small Cell Lung Cancer (NSCLC) / Other Cancers1
2Active Not RecruitingTreatmentCancer of Unknown Primary Site1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage Forms
FormRouteStrength
CapsuleOral150 mg/1
CapsuleOral150.000 mg
Capsule, coatedOral150 mg
CapsuleOral150 mg
Prices
Not Available
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)Region
US9278961No2016-03-082028-12-15US flag
US7888364No2011-02-152028-11-11US flag
US9790183No2017-10-172025-09-02US flag

Properties

State
Solid
Experimental Properties
PropertyValueSource
boiling point (°C)561.6°CSDS
water solubility0.1 μg/mL at pH 7FDA label
logP2.7 FDA label
pKa3.8FDA label
Predicted Properties
PropertyValueSource
Water Solubility0.00173 mg/mLALOGPS
logP4.22ALOGPS
logP3.93Chemaxon
logS-5.4ALOGPS
pKa (Strongest Acidic)13.5Chemaxon
pKa (Strongest Basic)3.7Chemaxon
Physiological Charge0Chemaxon
Hydrogen Acceptor Count4Chemaxon
Hydrogen Donor Count1Chemaxon
Polar Surface Area76.13 Å2Chemaxon
Rotatable Bond Count4Chemaxon
Refractivity107.81 m3·mol-1Chemaxon
Polarizability39.49 Å3Chemaxon
Number of Rings3Chemaxon
Bioavailability1Chemaxon
Rule of FiveYesChemaxon
Ghose FilterYesChemaxon
Veber's RuleNoChemaxon
MDDR-like RuleNoChemaxon
Predicted ADMET Features
PropertyValueProbability
Human Intestinal Absorption+0.9547
Blood Brain Barrier+0.9387
Caco-2 permeable+0.6048
P-glycoprotein substrateNon-substrate0.8443
P-glycoprotein inhibitor INon-inhibitor0.8663
P-glycoprotein inhibitor IINon-inhibitor0.9558
Renal organic cation transporterNon-inhibitor0.8925
CYP450 2C9 substrateNon-substrate0.6009
CYP450 2D6 substrateNon-substrate0.63
CYP450 3A4 substrateNon-substrate0.5083
CYP450 1A2 substrateNon-inhibitor0.6067
CYP450 2C9 inhibitorInhibitor0.9078
CYP450 2D6 inhibitorNon-inhibitor0.6638
CYP450 2C19 inhibitorInhibitor0.8515
CYP450 3A4 inhibitorInhibitor0.8452
CYP450 inhibitory promiscuityHigh CYP Inhibitory Promiscuity0.9282
Ames testNon AMES toxic0.8271
CarcinogenicityNon-carcinogens0.6746
BiodegradationNot ready biodegradable0.9956
Rat acute toxicity2.0840 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9973
hERG inhibition (predictor II)Non-inhibitor0.8224
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397)

Spectra

Mass Spec (NIST)
Not Available
Spectra
SpectrumSpectrum TypeSplash Key
MS/MS Spectrum - , positiveLC-MS/MSsplash10-00di-0212900000-190a5fdca2d781122e92
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSsplash10-00di-0030900000-2f4952455a6813195ed1
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSsplash10-014i-4000900000-a0864c8a02868ffa8ad6
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSsplash10-00di-0100900000-d1346d3e45d2b1bd1d46
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSsplash10-0159-7400900000-a639b349c47a05e2da0a
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSsplash10-001i-9002000000-d368d646e198ff199771
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSsplash10-0pdr-0968200000-108f56abfd6867e8d1bc
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]-187.35118
predicted
DeepCCS 1.0 (2019)
[M+H]+189.7092
predicted
DeepCCS 1.0 (2019)
[M+Na]+196.09016
predicted
DeepCCS 1.0 (2019)

Targets

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Details
1. Smoothened homolog
Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Antagonist
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. Sandhiya S, Melvin G, Kumar SS, Dkhar SA: The dawn of hedgehog inhibitors: Vismodegib. J Pharmacol Pharmacother. 2013 Jan;4(1):4-7. doi: 10.4103/0976-500X.107628. [Article]
  2. Aditya S, Rattan A: Vismodegib: A smoothened inhibitor for the treatment of advanced basal cell carcinoma. Indian Dermatol Online J. 2013 Oct;4(4):365-8. doi: 10.4103/2229-5178.120685. [Article]
  3. FDA Approved Drug Products: ERIVEDGE (vismodegib) capsules for oral use (March 2023) [Link]

Enzymes

Kind
Protein
Organism
Humans
Pharmacological action
No
Actions
Substrate
Inhibitor
Curator comments
Shown to be an inhibitor in vitro.
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
CYP2C9
Uniprot ID
P11712
Uniprot Name
Cytochrome P450 2C9
Molecular Weight
55627.365 Da
References
  1. Sandhiya S, Melvin G, Kumar SS, Dkhar SA: The dawn of hedgehog inhibitors: Vismodegib. J Pharmacol Pharmacother. 2013 Jan;4(1):4-7. doi: 10.4103/0976-500X.107628. [Article]
  2. Fellner C: Vismodegib (erivedge) for advanced Basal cell carcinoma. P T. 2012 Dec;37(12):670-82. [Article]
  3. FDA Approved Drug Products: ERIVEDGE (vismodegib) capsules for oral use (March 2023) [Link]
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. Sandhiya S, Melvin G, Kumar SS, Dkhar SA: The dawn of hedgehog inhibitors: Vismodegib. J Pharmacol Pharmacother. 2013 Jan;4(1):4-7. doi: 10.4103/0976-500X.107628. [Article]
  2. FDA Approved Drug Products: ERIVEDGE (vismodegib) capsules for oral use (March 2023) [Link]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inhibitor
Curator comments
Shown to be an inhibitor in vitro.
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. Fellner C: Vismodegib (erivedge) for advanced Basal cell carcinoma. P T. 2012 Dec;37(12):670-82. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inhibitor
Curator comments
Shown to be an inhibitor in vitro.
General Function
Steroid hydroxylase activity
Specific Function
Responsible for the metabolism of a number of therapeutic agents such as the anticonvulsant drug S-mephenytoin, omeprazole, proguanil, certain barbiturates, diazepam, propranolol, citalopram and im...
Gene Name
CYP2C19
Uniprot ID
P33261
Uniprot Name
Cytochrome P450 2C19
Molecular Weight
55930.545 Da
References
  1. Fellner C: Vismodegib (erivedge) for advanced Basal cell carcinoma. P T. 2012 Dec;37(12):670-82. [Article]

Carriers

Details
1. Serum albumin
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
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. FDA Approved Drug Products: ERIVEDGE (vismodegib) capsules for oral use (March 2023) [Link]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
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...
Gene Name
ORM1
Uniprot ID
P02763
Uniprot Name
Alpha-1-acid glycoprotein 1
Molecular Weight
23511.38 Da
References
  1. FDA Approved Drug Products: ERIVEDGE (vismodegib) capsules for oral use (March 2023) [Link]

Transporters

Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
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. Fellner C: Vismodegib (erivedge) for advanced Basal cell carcinoma. P T. 2012 Dec;37(12):670-82. [Article]
  2. FDA Approved Drug Products: ERIVEDGE (vismodegib) capsules for oral use (March 2023) [Link]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
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. Sandhiya S, Melvin G, Kumar SS, Dkhar SA: The dawn of hedgehog inhibitors: Vismodegib. J Pharmacol Pharmacother. 2013 Jan;4(1):4-7. doi: 10.4103/0976-500X.107628. [Article]

Drug created at January 04, 2013 21:48 / Updated at March 18, 2024 16:48