Cysteamine

Identification

Summary

Cysteamine is a cystine depleting agent used to treat the effects of cystinosis.

Brand Names
Cystagon, Cystaran, Procysbi
Generic Name
Cysteamine
DrugBank Accession Number
DB00847
Background

Cystinosis is a rare disease caused by mutations in the CTNS gene that encodes for cystinosin, a protein responsible for transporting cystine out of the cell lysosome. A defect in cystinosin function is followed by cystine accumulation throughout the body, especially the eyes and kidneys.2

Several preparations of cysteamine exist for the treatment of cystinosis manifestations, some in capsule form, and others in ophthalmic solution form.10,12 In particular, cystine deposits on the eye can cause significant discomfort throughout the day and require frequent treatment with eye drops, typically every waking hour.11

On August 25th 2020, the first ophthalmic solution for cystinosis requiring only 4 daily treatments was granted FDA approval.10 Cysteamine eye drops are a practical and effective option for those affected by ocular cystinosis. Marketed by Recordati Rare Diseases Inc., CYSTADROPS® reduce the burden of multiple frequent medications normally administered to those with cystinosis.9

Type
Small Molecule
Groups
Approved, Investigational
Structure
Weight
Average: 77.149
Monoisotopic: 77.029919919
Chemical Formula
C2H7NS
Synonyms
  • 2-amino-1-ethanethiol
  • 2-amino-ethanethiol
  • 2-aminoethanethiol
  • beta-aminoethanethiol
  • beta-Mercaptoethylamine
  • Cysteamine
  • MEA
  • Mercaptamina
  • Mercaptamine
  • Mercaptaminum
  • Thioethanolamine
  • β-aminoethylthiol
  • β-MEA
External IDs
  • L 1573
  • L-1573

Pharmacology

Indication

The bitartrate salt of cysteamine is used for the oral treatment of nephropathic cystinosis and cystinuria in adults and children ≥6 years old.12 The hydrochloride salt, used in eye drop preparations, is indicated for the treatment of corneal cystine crystal accumulation in patients with cystinosis.9,10

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Associated Conditions
Indication TypeIndicationCombined Product DetailsApproval LevelAge GroupPatient CharacteristicsDose Form
Management ofNephropathic cystinosis•••••••••••••••••• ••••••••••••••••• ••••••• •••••••
Treatment ofCorneal cystine crystal accumulation••••••••••••••••••••••
Contraindications & Blackbox Warnings
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Pharmacodynamics

Cystine accumulation is the cause of organ damage in cystinosis. Cysteamine prevents the accumulation of cystine crystals in the body and is specifically prescribed to prevent kidney and eye damage.4,9,12 Cysteamine converts cystine into a form that may easily exit cells, preventing harmful accumulation.10

Mechanism of action

Individuals born without the ability to metabolize cystine suffer from cystinosis, a rare genetic disorder characterized by the widespread accumulation of cystine crystals throughout the body and eye tissues. The cystine crystals may cause considerable damage, particularly in the renal tissues and corneal tissues. In some cases, renal failure can occur during childhood if the condition is left untreated. Other organs that may be affected by cystinosis include the CNS, thyroid, pancreas, muscle tissues, and gonads.2

Cysteamine converts cystine to cysteine and cysteine-cysteamine mixed disulfides, reducing the buildup of corneal cystine crystals.11 This drug participates in a thiol-disulfide interchange reaction with lysosomes, leading to cysteine exit from the lysosome in patients diagnosed with cystinosis.12

TargetActionsOrganism
ASomatostatin
binder
Humans
UCystine
cleavage
Humans
UNeuropeptide Y receptor type 2
other/unknown
Humans
Absorption

Orally administered cysteamine is absorbed in the gastrointestinal tract and reaches its maximum plasma concentration in about 1.4 hours, with some variation according to the type of formulation (delayed versus immediate-release).6,5,12 One pharmacokinetic study of adults with Cystic Fibrosis revealed a Cmax of 2.86 mg/L.6The maximum plasma concentration after administration of cysteamine eye drops is unknown, however, it is likely to be considerably lower than oral administration.10

According to prescribing information, the AUC 0-12 h for the delayed-release oral tablets is 99.26 ± 44.2 μmol*h/L with a Cmax of 27.70 ± 14.99 μmol/L.12

The AUC 0-12 for the immediate-release tablets is 192.00 ± 75.62 μmol*h/L with a Cmax of 37.72 ± 12.10 μmol/L.12

Volume of distribution

Cysteamine has a volume of distribution of about 129 L, according to one pharmacokinetic study.6 Prescribing information indicates a volume of distribution of 382 L for the delayed-release formulation and 198 L for the immediate-release preparation.12 It is known to cross the blood-brain barrier.8

Protein binding

Cysteamine is 52% plasma protein bound, and is mostly bound to albumin.12

Metabolism

There is limited information in the literature regarding the metabolism of cysteamine. This drug undergoes significant first-pass metabolism.8

Route of elimination

Not Available

Half-life

The half-life of cysteamine is about 3.7 hours.6

Clearance

The plasma clearance of cysteamine is about 1.2 - 1.4 L/min.12 One reference mentions a clearance of 89.9 L/h in patients with Cystic Fibrosis.6

Adverse Effects
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Toxicity

Two cases of human overdoses with cysteamine are recorded in the literature, according to prescribing information. In one case, vomiting was immediate after the administration of cysteamine, and the patient did not experience other symptoms. A 200 to 250 mg/kg dose was accidentally ingested by a healthy 13-month-old child. Vomiting and dehydration followed. A full recovery was made after hospitalization and the replenishment of fluids.13

There is no known antidote for an overdose with cysteamine. In the case of an overdose, provide supportive treatment, especially to the cardiovascular and respiratory systems. Hemodialysis may be useful in some cases due to the fact that cysteamine has poor plasma protein binding.13

Pathways
PathwayCategory
Taurine and Hypotaurine MetabolismMetabolic
Pantothenate and CoA BiosynthesisMetabolic
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
AlmasilateThe bioavailability of Cysteamine can be decreased when combined with Almasilate.
Aluminium phosphateThe bioavailability of Cysteamine can be decreased when combined with Aluminium phosphate.
Aluminum hydroxideThe bioavailability of Cysteamine can be decreased when combined with Aluminum hydroxide.
AsenapineAsenapine can cause an increase in the absorption of Cysteamine resulting in an increased serum concentration and potentially a worsening of adverse effects.
Bismuth subnitrateThe bioavailability of Cysteamine can be decreased when combined with Bismuth subnitrate.
Food Interactions
  • Take on an empty stomach. The delayed-release capsules should be taken at least 30 minutes before or 2 hours after a high-fat meal to ensure adequate exposure.
  • Take with or without food. The immediate release preparation can be taken with or without food.

Products

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Product Ingredients
IngredientUNIICASInChI Key
Cysteamine bitartrateQO84GZ3TST27761-19-9NSKJTUFFDRENDM-ZVGUSBNCSA-N
Cysteamine hydrochlorideIF1B771SVB156-57-0OGMADIBCHLQMIP-UHFFFAOYSA-N
International/Other Brands
Cystagon / Cystaran / Procysbi
Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
CystadropsSolution / drops3.8 mg/mlOphthalmicRecordati Rare Diseases2020-12-23Not applicableEU flag
CystadropsSolution / drops3.8 mg/mlOphthalmicRecordati Rare Diseases2020-12-23Not applicableEU flag
CystadropsSolution0.37 % w/wOphthalmicRecordati Rare Diseases Canada Inc2019-05-15Not applicableCanada flag
CystadropsSolution3.5 mg/1mLOphthalmicRECORDATI RARE DISEASES, INC.2020-08-19Not applicableUS flag
CystagonCapsule50 mg/1OralMylan Pharmaceuticals Inc.2005-04-11Not applicableUS flag

Categories

ATC Codes
A16AA04 — MercaptamineS01XA21 — Mercaptamine
Drug Categories
Chemical TaxonomyProvided by Classyfire
Description
This compound belongs to the class of organic compounds known as alkylthiols. These are organic compounds containing the thiol functional group linked to an alkyl chain.
Kingdom
Organic compounds
Super Class
Organosulfur compounds
Class
Thiols
Sub Class
Alkylthiols
Direct Parent
Alkylthiols
Alternative Parents
Organopnictogen compounds / Monoalkylamines / Hydrocarbon derivatives
Substituents
Aliphatic acyclic compound / Alkylthiol / Amine / Hydrocarbon derivative / Organic nitrogen compound / Organonitrogen compound / Organopnictogen compound / Primary aliphatic amine / Primary amine
Molecular Framework
Aliphatic acyclic compounds
External Descriptors
thiol, amine (CHEBI:17141) / Biogenic amines (C01678) / a thiol (CPD-239)
Affected organisms
  • Humans and other mammals

Chemical Identifiers

UNII
5UX2SD1KE2
CAS number
60-23-1
InChI Key
UFULAYFCSOUIOV-UHFFFAOYSA-N
InChI
InChI=1S/C2H7NS/c3-1-2-4/h4H,1-3H2
IUPAC Name
2-aminoethane-1-thiol
SMILES
NCCS

References

Synthesis Reference

Tethuharu Okazaki, Takeo Komukai, Saburo Uchikuga, "Process for preparing cysteamine-S-substituted compounds and derivatives thereof." U.S. Patent US4371472, issued September, 1969.

US4371472
General References
  1. Dohil R, Fidler M, Gangoiti JA, Kaskel F, Schneider JA, Barshop BA: Twice-daily cysteamine bitartrate therapy for children with cystinosis. J Pediatr. 2010 Jan;156(1):71-75.e1-3. doi: 10.1016/j.jpeds.2009.07.016. Epub . [Article]
  2. Elmonem MA, Veys KR, Soliman NA, van Dyck M, van den Heuvel LP, Levtchenko E: Cystinosis: a review. Orphanet J Rare Dis. 2016 Apr 22;11:47. doi: 10.1186/s13023-016-0426-y. [Article]
  3. Besouw M, Masereeuw R, van den Heuvel L, Levtchenko E: Cysteamine: an old drug with new potential. Drug Discov Today. 2013 Aug;18(15-16):785-92. doi: 10.1016/j.drudis.2013.02.003. Epub 2013 Feb 14. [Article]
  4. Cherqui S: Cysteamine therapy: a treatment for cystinosis, not a cure. Kidney Int. 2012 Jan;81(2):127-9. doi: 10.1038/ki.2011.301. [Article]
  5. Gangoiti JA, Fidler M, Cabrera BL, Schneider JA, Barshop BA, Dohil R: Pharmacokinetics of enteric-coated cysteamine bitartrate in healthy adults: a pilot study. Br J Clin Pharmacol. 2010 Sep;70(3):376-82. doi: 10.1111/j.1365-2125.2010.03721.x. [Article]
  6. Devereux G, Steele S, Griffiths K, Devlin E, Fraser-Pitt D, Cotton S, Norrie J, Chrystyn H, O'Neil D: An Open-Label Investigation of the Pharmacokinetics and Tolerability of Oral Cysteamine in Adults with Cystic Fibrosis. Clin Drug Investig. 2016 Aug;36(8):605-12. doi: 10.1007/s40261-016-0405-z. [Article]
  7. Langman CB, Greenbaum LA, Sarwal M, Grimm P, Niaudet P, Deschenes G, Cornelissen E, Morin D, Cochat P, Matossian D, Gaillard S, Bagger MJ, Rioux P: A randomized controlled crossover trial with delayed-release cysteamine bitartrate in nephropathic cystinosis: effectiveness on white blood cell cystine levels and comparison of safety. Clin J Am Soc Nephrol. 2012 Jul;7(7):1112-20. doi: 10.2215/CJN.12321211. Epub 2012 May 3. [Article]
  8. Dohil R, Cabrera BL, Gangoiti JA, Barshop BA, Rioux P: Pharmacokinetics of cysteamine bitartrate following intraduodenal delivery. Fundam Clin Pharmacol. 2014 Apr;28(2):136-43. doi: 10.1111/fcp.12009. Epub 2012 Oct 31. [Article]
  9. PRN News Wire: U.S. FDA Approves CYSTADROPS® (Cysteamine Ophthalmic Solution) 0.37%, A New Practical Treatment Option for the Ocular Manifestations of Cystinosis [Link]
  10. FDA Approved Products: Cystadrops (cysteamine solution 0.37%) for ophthalmic use [Link]
  11. FDA approved products: CYSTARAN (cysteamine 0.44%) for ophthalmic use [Link]
  12. FDA approved products: PROCYSBI (cysteamine bitartrate) delayed-release oral capsules [Link]
  13. FDA Approved Products: CYSTAGON® (cysteamine bitartrate) oral capsules [Link]
Human Metabolome Database
HMDB0002991
KEGG Drug
D03634
KEGG Compound
C01678
PubChem Compound
6058
PubChem Substance
46507730
ChemSpider
5834
BindingDB
7968
RxNav
3022
ChEBI
17141
ChEMBL
CHEMBL602
ZINC
ZINC000008034121
Therapeutic Targets Database
DAP001297
PharmGKB
PA449171
PDBe Ligand
DHL
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Cysteamine
PDB Entries
2y8d / 3q1l / 3som / 4cg4 / 4pa5 / 5apr / 5ej0 / 8cmb / 8cmh / 8d64
show 4 more
FDA label
Download (115 KB)
MSDS
Download (73.7 KB)

Clinical Trials

Clinical Trials
Clinical Trial & Rare Diseases Add-on Data Package
Explore 4,000+ rare diseases, orphan drugs & condition pairs, clinical trial why stopped data, & more. Preview package
PhaseStatusPurposeConditionsCountStart DateWhy Stopped100+ additional columns
Not AvailableCompletedNot AvailableCystinosis / Cystinosis, Nephropathic1somestatusstop reasonjust information to hide
Not AvailableCompletedTreatmentCorneal Cystine Crystals / Nephropathic Cyctinosis1somestatusstop reasonjust information to hide
Not AvailableCompletedTreatmentCystinosis1somestatusstop reasonjust information to hide
Not AvailableEnrolling by InvitationNot AvailableCystinosis, Nephropathic1somestatusstop reasonjust information to hide
Not AvailableRecruitingNot AvailableCystinosis1somestatusstop reasonjust information to hide

Pharmacoeconomics

Manufacturers
  • Mylan pharmaceuticals inc
Packagers
  • Mylan
Dosage Forms
FormRouteStrength
SolutionOphthalmic0.37 % w/w
SolutionOphthalmic3.5 mg/1mL
Solution / dropsOphthalmic3.8 MG/ML
SolutionOphthalmic3.8 mg
CapsuleOral150 mg/1
CapsuleOral150 MG
CapsuleOral50 MG
CapsuleOral50 mg/1
Capsule, coatedOral150 mg
Capsule, coatedOral50 mg
SolutionOphthalmic6.5 mg/1mL
Capsule, delayed releaseOral25 mg
Capsule, delayed releaseOral75 mg
GranuleOral300 mg
GranuleOral75 mg
Granule, delayed releaseOral300 mg/1
Granule, delayed releaseOral75 mg/1
Capsule, delayed release pelletsOral25 mg/1
Capsule, delayed release pelletsOral75 mg/1
Prices
Unit descriptionCostUnit
Cystagon 150 mg capsule1.28USD capsule
Cystagon 50 mg capsule0.44USD capsule
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)Region
US9192590Yes2015-11-242027-07-26US flag
US9198882Yes2015-12-012027-07-26US flag
US8026284Yes2011-09-272028-03-22US flag
US9233077Yes2016-01-122034-12-17US flag
US9173851Yes2015-11-032034-12-17US flag
US9925158Yes2018-03-272027-07-26US flag
US9925157Yes2018-03-272027-07-26US flag
US9925156Yes2018-03-272027-07-26US flag
US10143665Yes2018-12-042037-02-16US flag
US10328037Yes2019-06-252037-02-16US flag
US10548859Yes2020-02-042037-02-16US flag
US10905662Yes2021-02-022037-02-16US flag

Properties

State
Solid
Experimental Properties
PropertyValueSource
melting point (°C)67-71https://www.chemicalbook.com/ChemicalProductProperty_US_CB9337215.aspx
boiling point (°C)133.6±23.0 http://www.chemspider.com/Chemical-Structure.5834.html
water solubilityFreely soluble in water.https://www.chemicalbook.com/ChemicalProductProperty_US_CB9337215.aspx
logP0.1https://link.springer.com/article/10.1007/s40261-016-0405-z
pKa10.4https://link.springer.com/article/10.1007/s40261-016-0405-z
Predicted Properties
PropertyValueSource
Water Solubility23.5 mg/mLALOGPS
logP0.01ALOGPS
logP-0.42Chemaxon
logS-0.52ALOGPS
pKa (Strongest Acidic)9.42Chemaxon
pKa (Strongest Basic)10.4Chemaxon
Physiological Charge1Chemaxon
Hydrogen Acceptor Count1Chemaxon
Hydrogen Donor Count2Chemaxon
Polar Surface Area26.02 Å2Chemaxon
Rotatable Bond Count1Chemaxon
Refractivity22.39 m3·mol-1Chemaxon
Polarizability8.65 Å3Chemaxon
Number of Rings0Chemaxon
Bioavailability1Chemaxon
Rule of FiveYesChemaxon
Ghose FilterNoChemaxon
Veber's RuleYesChemaxon
MDDR-like RuleNoChemaxon
Predicted ADMET Features
PropertyValueProbability
Human Intestinal Absorption+0.9378
Blood Brain Barrier+0.7618
Caco-2 permeable+0.7461
P-glycoprotein substrateNon-substrate0.7
P-glycoprotein inhibitor INon-inhibitor0.9634
P-glycoprotein inhibitor IINon-inhibitor0.9637
Renal organic cation transporterNon-inhibitor0.751
CYP450 2C9 substrateNon-substrate0.9035
CYP450 2D6 substrateNon-substrate0.5713
CYP450 3A4 substrateNon-substrate0.8282
CYP450 1A2 substrateNon-inhibitor0.9046
CYP450 2C9 inhibitorNon-inhibitor0.9071
CYP450 2D6 inhibitorNon-inhibitor0.9231
CYP450 2C19 inhibitorNon-inhibitor0.9025
CYP450 3A4 inhibitorNon-inhibitor0.9396
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.8091
Ames testNon AMES toxic0.8488
CarcinogenicityNon-carcinogens0.5197
BiodegradationNot ready biodegradable0.7564
Rat acute toxicity2.2165 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.8358
hERG inhibition (predictor II)Non-inhibitor0.8686
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397)

Spectra

Mass Spec (NIST)
Download (7.29 KB)
Spectra
SpectrumSpectrum TypeSplash Key
GC-MS Spectrum - GC-EI-TOF (Pegasus III TOF-MS system, Leco; GC 6890, Agilent Technologies) (3 TMS)GC-MSsplash10-00di-1900000000-287334efed4c27d47e62
GC-MS Spectrum - GC-EI-TOF (Pegasus III TOF-MS system, Leco; GC 6890, Agilent Technologies) (3 TMS)GC-MSsplash10-00di-1900000000-e26f666cab18d523e475
GC-MS Spectrum - GC-EI-TOF (Pegasus III TOF-MS system, Leco; GC 6890, Agilent Technologies) (3 TMS)GC-MSsplash10-00di-7900000000-25e27a3413a3e9bd6e86
GC-MS Spectrum - GC-MS (3 TMS)GC-MSsplash10-00dr-3900000000-5f3c0dc6b99382c852e2
Predicted GC-MS Spectrum - GC-MSPredicted GC-MSsplash10-003u-9000000000-48a76c3cb5971165dc16
GC-MS Spectrum - GC-EI-TOFGC-MSsplash10-00di-1900000000-287334efed4c27d47e62
GC-MS Spectrum - GC-EI-TOFGC-MSsplash10-00di-1900000000-e26f666cab18d523e475
GC-MS Spectrum - GC-EI-TOFGC-MSsplash10-00di-7900000000-25e27a3413a3e9bd6e86
GC-MS Spectrum - GC-MSGC-MSsplash10-00dr-3900000000-5f3c0dc6b99382c852e2
GC-MS Spectrum - GC-MSGC-MSsplash10-00dr-3900000000-5f3c0dc6b99382c852e2
GC-MS Spectrum - GC-EI-TOFGC-MSsplash10-00di-2900000000-ba8ae281d3d77ff202c1
MS/MS Spectrum - Quattro_QQQ 10V, Positive (Annotated)LC-MS/MSsplash10-03di-9000000000-0fdf5bdcf8a4a1bf9afb
MS/MS Spectrum - Quattro_QQQ 25V, Positive (Annotated)LC-MS/MSsplash10-03di-9000000000-f99f2f10c6728595d6ea
MS/MS Spectrum - Quattro_QQQ 40V, Positive (Annotated)LC-MS/MSsplash10-01t9-9000000000-fa7f96e00debe1bebf70
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSsplash10-03di-9000000000-438f302ebc492730e9e5
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSsplash10-004i-9000000000-5207c5cd8c707da5077c
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSsplash10-004i-9000000000-9133df934b3577a66e30
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSsplash10-03di-9000000000-c3610d35e5672bb4a916
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSsplash10-0a59-9000000000-b37e476c82cba6f0af41
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSsplash10-03di-9000000000-fe26258cb83c047f9da6
1H NMR Spectrum1D NMRNot Applicable
Predicted 1H NMR Spectrum1D NMRNot Applicable
Predicted 13C NMR Spectrum1D NMRNot Applicable
[1H,13C] 2D NMR Spectrum2D NMRNot Applicable
Chromatographic Properties
Collision Cross Sections (CCS)
AdductCCS Value (Å2)Source typeSource
[M-H]-100.768434
predicted
DarkChem Lite v0.1.0
[M-H]-100.730434
predicted
DarkChem Lite v0.1.0
[M-H]-117.33682
predicted
DeepCCS 1.0 (2019)
[M+H]+102.378734
predicted
DarkChem Lite v0.1.0
[M+H]+102.355334
predicted
DarkChem Lite v0.1.0
[M+H]+119.17246
predicted
DeepCCS 1.0 (2019)
[M+Na]+101.418534
predicted
DarkChem Lite v0.1.0
[M+Na]+101.527934
predicted
DarkChem Lite v0.1.0
[M+Na]+126.305214
predicted
DeepCCS 1.0 (2019)

Targets

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Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Binder
General Function
Inhibits the secretion of pituitary hormones, including that of growth hormone/somatotropin (GH1), PRL, ACTH, luteinizing hormone (LH) and TSH. Also impairs ghrelin- and GnRH-stimulated secretion of GH1 and LH; the inhibition of ghrelin-stimulated secretion of GH1 can be further increased by neuronostatin
Specific Function
hormone activity
Gene Name
SST
Uniprot ID
P61278
Uniprot Name
Somatostatin
Molecular Weight
12735.395 Da
References
  1. Zhou Y, Zhang Y, Zhao D, Yu X, Shen X, Zhou Y, Wang S, Qiu Y, Chen Y, Zhu F: TTD: Therapeutic Target Database describing target druggability information. Nucleic Acids Res. 2024 Jan 5;52(D1):D1465-D1477. doi: 10.1093/nar/gkad751. [Article]
Kind
Small molecule
Organism
Humans
Pharmacological action
Unknown
Actions
Cleavage
References
  1. Omran Z, Kay G, Di Salvo A, Knott RM, Cairns D: PEGylated derivatives of cystamine as enhanced treatments for nephropathic cystinosis. Bioorg Med Chem Lett. 2011 Jan 1;21(1):45-7. doi: 10.1016/j.bmcl.2010.11.085. Epub 2010 Nov 21. [Article]
  2. FDA approved products: PROCYSBI (cysteamine bitartrate) delayed-release oral capsules [Link]
  3. PRN News Wire: U.S. FDA Approves CYSTADROPS® (Cysteamine Ophthalmic Solution) 0.37%, A New Practical Treatment Option for the Ocular Manifestations of Cystinosis [Link]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Other/unknown
Curator comments
Data for this target action are limited to animal studies and relevance to humans is unknown.
General Function
Receptor for neuropeptide Y and peptide YY. The rank order of affinity of this receptor for pancreatic polypeptides is PYY > NPY > PYY (3-36) > NPY (2-36) > [Ile-31, Gln-34] PP > [Leu-31, Pro-34] NPY > PP, [Pro-34] PYY and NPY free acid
Specific Function
calcium channel regulator activity
Gene Name
NPY2R
Uniprot ID
P49146
Uniprot Name
Neuropeptide Y receptor type 2
Molecular Weight
42730.69 Da
References
  1. Li W, Hexum TD: Cysteamine selectively enhances neuropeptide Y2 receptor binding activity. Biochem Biophys Res Commun. 1992 Apr 15;184(1):380-6. [Article]

Enzymes

Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Part of the host defense system of polymorphonuclear leukocytes. It is responsible for microbicidal activity against a wide range of organisms. In the stimulated PMN, MPO catalyzes the production of hypohalous acids, primarily hypochlorous acid in physiologic situations, and other toxic intermediates that greatly enhance PMN microbicidal activity (PubMed:9922160). Mediates the proteolytic cleavage of alpha-1-microglobulin to form t-alpha-1-microglobulin, which potently inhibits oxidation of low-density lipoprotein particles and limits vascular damage (PubMed:25698971)
Specific Function
chromatin binding
Gene Name
MPO
Uniprot ID
P05164
Uniprot Name
Myeloperoxidase
Molecular Weight
83867.71 Da
References
  1. Svensson BE: Abilities of peroxidases to catalyse peroxidase-oxidase oxidation of thiols. Biochem J. 1988 Dec 15;256(3):757-62. [Article]
  2. Svensson BE, Graslund A, Strom G, Moldeus P: Thiols as peroxidase substrates. Free Radic Biol Med. 1993 Feb;14(2):167-75. [Article]
  3. Svensson BE, Lindvall S: Myeloperoxidase-oxidase oxidation of cysteamine. Biochem J. 1988 Jan 15;249(2):521-30. [Article]

Carriers

Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Binder
General Function
Binds water, Ca(2+), Na(+), K(+), fatty acids, hormones, bilirubin and drugs (Probable). Its main function is the regulation of the colloidal osmotic pressure of blood (Probable). Major zinc transporter in plasma, typically binds about 80% of all plasma zinc (PubMed:19021548). Major calcium and magnesium transporter in plasma, binds approximately 45% of circulating calcium and magnesium in plasma (By similarity). Potentially has more than two calcium-binding sites and might additionally bind calcium in a non-specific manner (By similarity). The shared binding site between zinc and calcium at residue Asp-273 suggests a crosstalk between zinc and calcium transport in the blood (By similarity). The rank order of affinity is zinc > calcium > magnesium (By similarity). Binds to the bacterial siderophore enterobactin and inhibits enterobactin-mediated iron uptake of E.coli from ferric transferrin, and may thereby limit the utilization of iron and growth of enteric bacteria such as E.coli (PubMed:6234017). Does not prevent iron uptake by the bacterial siderophore aerobactin (PubMed:6234017)
Specific Function
antioxidant activity
Gene Name
ALB
Uniprot ID
P02768
Uniprot Name
Albumin
Molecular Weight
69365.94 Da
References
  1. FDA approved products: PROCYSBI (cysteamine bitartrate) delayed-release oral capsules [Link]

Drug created at June 13, 2005 13:24 / Updated at August 26, 2024 19:23