Sevelamer

Identification

Name
Sevelamer
Accession Number
DB00658
Description

Sevelamer is a phosphate binding drug used to prevent hyperphosphataemia in patients with chronic renal failure. It is marketed by Genzyme under the trade name Renagel.

Type
Small Molecule
Groups
Approved
Structure
Thumb
Weight
Average: 149.619
Monoisotopic: 149.060741718
Chemical Formula
C6H12ClNO
Synonyms
  • Sevelamer
  • Sévélamer
  • Sevelamero
  • Sevelamerum
External IDs
  • GT 16026 A
  • GT 335-012

Pharmacology

Indication

For the control of serum phosphorus in patients with Chronic Kidney Disease (CKD) on hemodialysis.

Associated Conditions
Contraindications & Blackbox Warnings
Learn about our commercial Contraindications & Blackbox Warnings data.
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Pharmacodynamics

Patients with end-stage renal disease (ESRD) retain phosphorus and can develop hyperphosphatemia. High serum phosphorus can precipitate serum calcium resulting in ectopic calcification. When the product of serum calcium and phosphorus concentrations (Ca x P) exceeds 55 mg2/dL2, there is an increased risk that ectopic calcification will occur. Hyperphosphatemia plays a role in the development of secondary hyperparathyroidism in renal insufficiency. An increase in parathyroid hormone (PTH) levels is characteristic of patients with chronic renal failure. Increased levels of PTH can lead to osteitis fibrosa, a bone disease. A decrease in serum phosphorus may decrease serum PTH levels. Treatment of hyperphosphatemia includes reduction in dietary intake of phosphate, inhibition of intestinal phosphate absorption with phosphate binders, and removal of phosphate with dialysis. Sevelamer taken with meals has been shown to decrease serum phosphorus concentrations in patients with ESRD who are on hemodialysis. In vitro studies have shown that the capsule and tablet formulations bind phosphate to a similar extent. Sevelamer treatment also results in a lowering of low-density lipoprotein (LDL) and total serum cholesterol levels.

Mechanism of action

Sevelamer prevents hyperphosphatemia by binding to dietary phosphate in the gut, preventing its absorption and thus decreasing serum parathyroid hormone levels.

TargetActionsOrganism
APhosphate
binder
Humans
Absorption

Not absorbed following oral administration, however no absorption studies have been performed in patients with renal disease. Sevelamer may bind to dietary phosphates and prevent its gastrointestinal absorption when sevelamer is administered in combination with food.

Volume of distribution
Not Available
Protein binding
Not Available
Metabolism
Not Available
Route of elimination
Not Available
Half-life
Not Available
Clearance
Not Available
Adverse Effects
Learn about our commercial Adverse Effects data.
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Toxicity

Sevelamer has been given to normal healthy volunteers in doses of up to 14 grams per day for eight days with no adverse effects. Sevelamer has been given in average doses up to 13 grams per day to hemodialysis patients. There are no reported overdosages of sevelamer in patients. Since sevelamer is not absorbed, the risk of systemic toxicity is low.

Affected organisms
  • Humans and other mammals
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
AceclofenacSevelamer can cause a decrease in the absorption of Aceclofenac resulting in a reduced serum concentration and potentially a decrease in efficacy.
AcemetacinSevelamer can cause a decrease in the absorption of Acemetacin resulting in a reduced serum concentration and potentially a decrease in efficacy.
AcenocoumarolSevelamer can cause a decrease in the absorption of Acenocoumarol resulting in a reduced serum concentration and potentially a decrease in efficacy.
AcetazolamideSevelamer can cause a decrease in the absorption of Acetazolamide resulting in a reduced serum concentration and potentially a decrease in efficacy.
Acetyl sulfisoxazoleSevelamer can cause a decrease in the absorption of Acetyl sulfisoxazole resulting in a reduced serum concentration and potentially a decrease in efficacy.
AcetyldigitoxinSevelamer can cause a decrease in the absorption of Acetyldigitoxin resulting in a reduced serum concentration and potentially a decrease in efficacy.
Acetylsalicylic acidSevelamer can cause a decrease in the absorption of Acetylsalicylic acid resulting in a reduced serum concentration and potentially a decrease in efficacy.
AlclofenacSevelamer can cause a decrease in the absorption of Alclofenac resulting in a reduced serum concentration and potentially a decrease in efficacy.
AlfacalcidolThe serum concentration of Alfacalcidol can be decreased when it is combined with Sevelamer.
AminophenazoneSevelamer can cause a decrease in the absorption of Aminophenazone resulting in a reduced serum concentration and potentially a decrease in efficacy.
Additional Data Available
  • Extended Description
    Extended Description

    Extended description of the mechanism of action and particular properties of each drug interaction.

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  • Severity
    Severity

    A severity rating for each drug interaction, from minor to major.

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  • Evidence Level
    Evidence Level

    A rating for the strength of the evidence supporting each drug interaction.

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  • Action
    Action

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Food Interactions
  • Take with food.

Products

Product Ingredients
IngredientUNIICASInChI Key
Sevelamer carbonate9YCX42I8IU845273-93-0PADGNZFOVSZIKZ-UHFFFAOYSA-N
Sevelamer hydrochlorideGLS2PGI8QG152751-57-0KHNXRSIBRKBJDI-UHFFFAOYSA-N
Product Images
International/Other Brands
Phosblock (Kyowa Hakko Kirin)
Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
Intelli-sevelamerTabletOralIntellipharm IncNot applicableNot applicableCanada
RenagelTablet800 mg/1OralCardinal Health2008-06-062017-11-30Us58468 0021 01 nlmimage10 cb1c6593
RenagelTablet800 mg/1OralPhysicians Total Care, Inc.2006-06-302011-06-30Us
RenagelTablet800 mg/1OralDoh Central Pharmacy2009-07-01Not applicableUs53808 077720180913 8702 1t9hnek
RenagelTablet400 mg/1OralCardinal Health2008-06-062014-07-31Us
RenagelTablet800 mgOralSanofi Aventis2001-11-21Not applicableCanada
RenagelTablet400 mgOralSanofi Genzyme, a Division of Sanofi Aventis Canada Inc2001-11-212005-08-08Canada
RenagelTablet800 mg/1OralAphena Pharma Solutions Tennessee, Inc.2008-06-06Not applicableUs
RenagelTablet800 mg/1OralGenzyme Corporation2008-06-06Not applicableUs58468 002120180907 15195 1a6on42
RenagelTablet400 mg/1OralCarilion Materials Management2008-06-06Not applicableUs
Additional Data Available
  • Application Number
    Application Number

    A unique ID assigned by the FDA when a product is submitted for approval by the labeller.

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  • Product Code
    Product Code

    A governmentally-recognized ID which uniquely identifies the product within its regulatory market.

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Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
Accel-sevelamerTabletOralAccel Pharma Inc2017-11-08Not applicableCanada
Sevelamer CarbonatePowder, for suspension2400 mg/1OralAurobindo Pharma Limited2017-06-13Not applicableUs
Sevelamer CarbonateTablet, film coated800 mg/1OralREMEDYREPACK INC.2019-12-17Not applicableUs
Sevelamer CarbonatePowder, for suspension2.4 g/1OralWinthrop U.S.2018-01-01Not applicableUs
Sevelamer carbonateTablet, film coated800 mg/1OralREMEDYREPACK INC.2017-12-142020-05-07Us
Sevelamer CarbonateTablet, film coated800 mg/1OralKAISER FOUNDATION HOSPITALS2017-12-182018-09-30Us
Sevelamer carbonateTablet, film coated800 mg/1OralUnit Dose Services2017-10-26Not applicableUs
Sevelamer carbonateTablet, film coated800 mg/1OralInvaGen Pharmaceuticals Inc.2017-10-26Not applicableUs
Sevelamer CarbonateTablet, film coated800 mg/1OralGolden State Medical Supply, Inc.2017-10-20Not applicableUs
Sevelamer CarbonateTablet, film coated800 mg/1OralImpax Generics2017-10-232019-12-31Us
Additional Data Available
  • Application Number
    Application Number

    A unique ID assigned by the FDA when a product is submitted for approval by the labeller.

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  • Product Code
    Product Code

    A governmentally-recognized ID which uniquely identifies the product within its regulatory market.

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Categories

ATC Codes
V03AE02 — Sevelamer
Drug Categories
Chemical TaxonomyProvided by Classyfire
Description
This compound belongs to the class of organic compounds known as epoxides. These are compounds containing a cyclic ether with three ring atoms(one oxygen and two carbon atoms).
Kingdom
Organic compounds
Super Class
Organoheterocyclic compounds
Class
Epoxides
Sub Class
Not Available
Direct Parent
Epoxides
Alternative Parents
Oxacyclic compounds / Dialkyl ethers / Organopnictogen compounds / Organochlorides / Monoalkylamines / Hydrocarbon derivatives / Alkyl chlorides
Substituents
Aliphatic heteromonocyclic compound / Alkyl chloride / Alkyl halide / Amine / Dialkyl ether / Ether / Hydrocarbon derivative / Organic nitrogen compound / Organic oxygen compound / Organochloride
Molecular Framework
Not Available
External Descriptors
Not Available

Chemical Identifiers

UNII
941N5DUU5C
CAS number
52757-95-6
InChI Key
ZNSIZMQNQCNRBW-UHFFFAOYSA-N
InChI
InChI=1S/C3H5ClO.C3H7N/c4-1-3-2-5-3;1-2-3-4/h3H,1-2H2;2H,1,3-4H2
IUPAC Name
2-(chloromethyl)oxirane; prop-2-en-1-amine
SMILES
NCC=C.ClCC1CO1

References

Synthesis Reference

Deepak Anant Hedge, Varsha Shashank Choudhary, Venkatasubramanian Radhakrjshnan Tarur, Dhananjay Govind Sathe, Harish Kashinath Mondkar, Samadhan Daulat Patil, Sasikumar Mohan Thoovara, Yogesh Sharad Bhide, "Process for the Preparation of Sevelamer Hydrochloride and Formulation Thereof." U.S. Patent US20090280178, issued November 12, 2009.

US20090280178
General References
Not Available
Human Metabolome Database
HMDB0014796
KEGG Drug
D01983
PubChem Compound
3085017
PubChem Substance
46505951
ChemSpider
2341997
RxNav
214824
ChEMBL
CHEMBL1201798
PharmGKB
PA164781197
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Sevelamer
AHFS Codes
  • 40:18.19 — Phosphate-removing Agents
FDA label
Download (36.4 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
4Active Not RecruitingTreatmentEnd Stage Renal Disease (ESRD) / Hyperphosphataemia1
4CompletedPreventionVascular Diseases1
4CompletedPreventionWe Investigated the Relationship Between Plasma FGF23 Levels and Endothelial Dysfunction in a Sizable Series of Incident Stage 3-4 CKD Patients1
4CompletedTreatmentArteriosclerosis / Calcinosis / Hyperparathyroidism, Secondary1
4CompletedTreatmentCardiovascular Events / Hemodialysis Treatment / Hyperphosphataemia1
4CompletedTreatmentChronic Kidney Disease (CKD)3
4Not Yet RecruitingOtherSmallpox1
4TerminatedPreventionChronic Kidney Disease (CKD)1
3Active Not RecruitingTreatmentChronic Kidney Disease Requiring Chronic Dialysis / Hyperphosphataemia1
3CompletedPreventionHyperphosphataemia / Renal Failure1

Pharmacoeconomics

Manufacturers
  • Genzyme corp
  • Genzyme Corporation
Packagers
  • Atlantic Biologicals Corporation
  • Cardinal Health
  • Genzyme Inc.
  • Heartland Repack Services LLC
  • Murfreesboro Pharmaceutical Nursing Supply
  • Pharma Pac LLC
  • Physicians Total Care Inc.
  • Prepak Systems Inc.
  • Remedy Repack
  • Resource Optimization and Innovation LLC
  • Southwood Pharmaceuticals
  • Tya Pharmaceuticals
  • Vangard Labs Inc.
  • Warner Chilcott Co. Inc.
  • Watson Pharmaceuticals
Dosage Forms
FormRouteStrength
TabletOral
CapsuleOral403 mg
TabletOral400 mg/1
TabletOral400 mg
TabletOral800 mg/1
TabletOral800 mg
Powder, for suspensionOral0.8 g
Powder, for suspensionOral1.6 g
Powder, for suspensionOral2.4 g
Tablet, film coatedOral800 mg
Tablet, film coatedOral800 mg/1
Powder, for suspensionOral0.8 g/1
Powder, for suspensionOral2.4 g/1
Powder, for suspensionOral2400 mg/1
Powder, for suspensionOral800 mg/1
Tablet, film coatedOral400 mg/1
Tablet, film coatedParenteral800 mg/1
Prices
Unit descriptionCostUnit
Renagel 800 mg tablet2.41USD tablet
Renvela 800 mg tablet2.17USD tablet
Renagel 400 mg tablet1.66USD tablet
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)Region
US5496545No1996-03-052013-08-11Us
CA2310960No2003-05-272014-08-10Canada
CA2169356No2000-07-042014-08-10Canada
US7985418No2011-07-262025-10-27Us
US6733780No2004-05-112020-10-18Us
US9095509No2015-08-042030-12-06Us
Additional Data Available
  • Filed On
    Filed On

    The date on which a patent was filed with the relevant government.

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Properties

State
Solid
Experimental Properties
PropertyValueSource
water solubilityInsolubleNot Available
logP0.559Not Available
Predicted Properties
PropertyValueSource
logP0.68ChemAxon
pKa (Strongest Basic)-4.2ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count1ChemAxon
Hydrogen Donor Count0ChemAxon
Polar Surface Area12.53 Å2ChemAxon
Rotatable Bond Count2ChemAxon
Refractivity20.06 m3·mol-1ChemAxon
Polarizability8.38 Å3ChemAxon
Number of Rings1ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterNoChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleNoChemAxon
Predicted ADMET Features
PropertyValueProbability
Human Intestinal Absorption+0.9908
Blood Brain Barrier+0.9723
Caco-2 permeable+0.5783
P-glycoprotein substrateNon-substrate0.7654
P-glycoprotein inhibitor INon-inhibitor0.921
P-glycoprotein inhibitor IINon-inhibitor0.9399
Renal organic cation transporterNon-inhibitor0.7531
CYP450 2C9 substrateNon-substrate0.8823
CYP450 2D6 substrateNon-substrate0.8029
CYP450 3A4 substrateNon-substrate0.7617
CYP450 1A2 substrateNon-inhibitor0.5084
CYP450 2C9 inhibitorNon-inhibitor0.7543
CYP450 2D6 inhibitorNon-inhibitor0.839
CYP450 2C19 inhibitorNon-inhibitor0.5583
CYP450 3A4 inhibitorNon-inhibitor0.8711
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.6708
Ames testAMES toxic0.9498
CarcinogenicityCarcinogens 0.5468
BiodegradationNot ready biodegradable0.889
Rat acute toxicity2.9282 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.7403
hERG inhibition (predictor II)Non-inhibitor0.8883
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
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSNot Available

Targets

Kind
Small molecule
Organism
Humans
Pharmacological action
Yes
Actions
Binder
References
  1. Cannata-Andia JB, Rodriguez-Garcia M, Roman-Garcia P, Tunon-le Poultel D, Lopez-Hernandez F, Rodriguez-Puyol D: New therapies: calcimimetics, phosphate binders and vitamin D receptor activators. Pediatr Nephrol. 2010 Apr;25(4):609-16. doi: 10.1007/s00467-010-1462-9. Epub 2010 Feb 12. [PubMed:20151157]
  2. Novak JE, Szczech LA: Phosphate binders in chronic kidney disease and end-stage renal disease: a patient-centered approach. Semin Dial. 2009 Jan-Feb;22(1):56-63. doi: 10.1111/j.1525-139X.2008.00514.x. Epub 2008 Oct 16. [PubMed:19000107]
  3. Salusky IB: A new era in phosphate binder therapy: what are the options? Kidney Int Suppl. 2006 Dec;(105):S10-5. [PubMed:17136110]
  4. Schucker JJ, Ward KE: Hyperphosphatemia and phosphate binders. Am J Health Syst Pharm. 2005 Nov 15;62(22):2355-61. [PubMed:16278327]

Drug created on June 13, 2005 07:24 / Updated on August 10, 2020 08:11

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