Patiromer

Identification

Summary

Patiromer is a potassium binder indicated for the treatment of hyperkalemia.

Brand Names
Veltassa
Generic Name
Patiromer
DrugBank Accession Number
DB09263
Background

Patiromer is a powder for suspension in water for oral administration, approved in the U.S. as Veltassa in October, 2015. Patiromer is supplied as patiromer sorbitex calcium which consists of the active moiety, patiromer, a non-absorbed potassium-binding polymer, and a calcium-sorbitol counterion. Each gram of patiromer is equivalent to a nominal amount of 2 grams of patiromer sorbitex calcium. The chemical name for patiromer sorbitex calcium is cross-linked polymer of calcium 2-fluoroprop-2-enoate with diethenylbenzene and octa-1,7-diene, combination with D-glucitol. Patiromer sorbitex calcium is an amorphous, free-flowing powder that is composed of individual spherical beads.

Type
Small Molecule
Groups
Approved, Investigational
Synonyms
  • Patiromer
  • Patiromer FOS
External IDs
  • RLY5016

Pharmacology

Indication

For the treatment of hyperkalemia.

Pharmacology
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Associated Conditions
Contraindications & Blackbox Warnings
Contraindications
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Pharmacodynamics

In clinical studies, patiromer decreased systemic exposure of some coadministered oral medications. Binding of patiromer to other oral medications could cause decreased gastrointestinal absorption and loss of efficacy when taken close to the time patiromer is administered. Administer oral medications at least 3 hours before or 3 hours after patiromer.

Mechanism of action

Patiromer is a non-absorbed, cation exchange polymer that contains a calcium-sorbitol counterion. It increases fecal potassium excretion through binding of potassium in the lumen of the gastrointestinal tract. Binding of potassium reduces the concentration of free potassium in the gastrointestinal lumen, resulting in a reduction of serum potassium levels.

TargetActionsOrganism
APotassium
binder
Humans
Absorption

In radiolabeled studies in cats and dogs, patiromer was not systemically absorbed.

Volume of distribution

Not Available

Protein binding

Not Available

Metabolism
Not Available
Route of elimination

Excretion in feces.

Half-life

Not Available

Clearance

Not Available

Adverse Effects
Medicalerrors
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Toxicity

Not Available

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
CiprofloxacinPatiromer can cause a decrease in the absorption of Ciprofloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.
LevothyroxinePatiromer can cause a decrease in the absorption of Levothyroxine resulting in a reduced serum concentration and potentially a decrease in efficacy.
MetforminPatiromer can cause a decrease in the absorption of Metformin resulting in a reduced serum concentration and potentially a decrease in efficacy.
Interactions
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Food Interactions
  • Take with or without food.

Products

Products
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Product Ingredients
IngredientUNIICASInChI Key
Patiromer sorbitex calcium0LB9J2797DNot AvailableNot applicable
Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
VeltassaPowder, for suspensionOralVifor Fresenius Medical Care Renal Pharma France2020-12-16Not applicableEU flag
VeltassaPowder, for suspensionOralVifor Fresenius Medical Care Renal Pharma France2020-12-16Not applicableEU flag
VeltassaPowder, for suspension16.8 gOralVifor Fresenius Medical Care Renal Pharma Ltd2019-11-27Not applicableCanada flag
VeltassaPowder, for suspension16.8 g/1OralRelypsa, Inc.2015-10-23Not applicableUS flag
VeltassaPowder, for suspensionOralVifor Fresenius Medical Care Renal Pharma France2020-12-16Not applicableEU flag
VeltassaPowder, for suspensionOralVifor Fresenius Medical Care Renal Pharma France2020-12-16Not applicableEU flag
VeltassaPowder, for suspensionOralVifor Fresenius Medical Care Renal Pharma France2020-12-16Not applicableEU flag
VeltassaPowder, for suspensionOralVifor Fresenius Medical Care Renal Pharma France2020-12-16Not applicableEU flag
VeltassaPowder, for suspension8.4 gOralVifor Fresenius Medical Care Renal Pharma Ltd2020-03-09Not applicableCanada flag
VeltassaPowder, for suspension8.4 g/1OralRelypsa, Inc.2015-10-23Not applicableUS flag

Categories

Drug Categories
Classification
Not classified
Affected organisms
  • Humans and other mammals

Chemical Identifiers

UNII
1FQ2RY5YHH
CAS number
1260643-52-4
InChI Key
Not Available
InChI
Not Available
IUPAC Name
Not Available
SMILES
Not Available

References

General References
  1. Pitt B, Anker SD, Bushinsky DA, Kitzman DW, Zannad F, Huang IZ: Evaluation of the efficacy and safety of RLY5016, a polymeric potassium binder, in a double-blind, placebo-controlled study in patients with chronic heart failure (the PEARL-HF) trial. Eur Heart J. 2011 Apr;32(7):820-8. doi: 10.1093/eurheartj/ehq502. Epub 2011 Jan 5. [PubMed:21208974]
  2. Montaperto AG, Gandhi MA, Gashlin LZ, Symoniak MR: Patiromer: a clinical review. Curr Med Res Opin. 2016;32(1):155-64. doi: 10.1185/03007995.2015.1106935. Epub 2015 Nov 19. [PubMed:26456884]
KEGG Drug
D10148
PubChem Substance
347910426
RxNav
1716203
ChEMBL
CHEMBL2107875
Wikipedia
Patiromer
AHFS Codes
  • 40:18.18 — Potassium-removing Agents
FDA label
Download (352 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
4Active Not RecruitingTreatmentChronic Kidney Disease (CKD) / Hyperkalemia1
4CompletedTreatmentChronic Renal Failure (CRF)1
4CompletedTreatmentHyperkalemia1
4CompletedTreatmentHyperkalemia / Transplant, Kidney1
4Enrolling by InvitationPreventionEnd Stage Renal Disease (ESRD) / Hyperkalemia1
4Not Yet RecruitingTreatmentCongestive Heart Failure (CHF)1
4RecruitingTreatmentAcute Hyperkalemia / Oral Potassium Binders1
4RecruitingTreatmentHyperkalemia1
4Unknown StatusTreatmentHyperkalemia / Type 2 Diabetes Mellitus1
3CompletedTreatmentChronic Kidney Disease (CKD) / Hyperkalemia1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage Forms
FormRouteStrength
Powder, for suspensionOral
Powder, for suspensionOral16.8 g
Powder, for suspensionOral16.8 g/1
Powder, for suspensionOral25.2 g/1
Powder, for suspensionOral25.2 g
Powder, for suspensionOral8.4 g/1
Powder, for suspensionOral8.4 g
Prices
Not Available
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)Region
US8475780No2013-07-022024-03-30US flag
US8216560No2012-07-102027-03-14US flag
US8889115No2014-11-182024-03-30US flag
US8337824No2012-12-252030-05-29US flag
US7556799No2009-07-072025-02-27US flag
US8778324No2014-07-152024-03-30US flag
US8287847No2012-10-162024-03-30US flag
US8282913No2012-10-092026-03-11US flag
US8147873No2012-04-032026-03-11US flag
US9492476No2016-11-152033-10-08US flag
US9925212No2018-03-272033-10-08US flag
US10485821No2019-11-262024-03-30US flag

Properties

State
Solid
Experimental Properties
Not Available
Predicted Properties
Not Available
Predicted ADMET Features
Not Available

Spectra

Mass Spec (NIST)
Not Available
Spectra
Not Available

Targets

Drugtargets
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Kind
Small molecule
Organism
Humans
Pharmacological action
Yes
Actions
Binder
References
  1. van der Meer P, van Veldhuisen DJ: To bind or not to bind: potassium-lowering drugs in heart failure. Eur Heart J. 2011 Apr;32(7):791-2. doi: 10.1093/eurheartj/ehr058. Epub 2011 Mar 7. [PubMed:21383002]
  2. Pitt B, Anker SD, Bushinsky DA, Kitzman DW, Zannad F, Huang IZ: Evaluation of the efficacy and safety of RLY5016, a polymeric potassium binder, in a double-blind, placebo-controlled study in patients with chronic heart failure (the PEARL-HF) trial. Eur Heart J. 2011 Apr;32(7):820-8. doi: 10.1093/eurheartj/ehq502. Epub 2011 Jan 5. [PubMed:21208974]

Drug created on October 27, 2015 15:43 / Updated on May 06, 2021 06:19