Identification

Name
Patiromer
Accession Number
DB09263
Type
Small Molecule
Groups
Approved, Investigational
Description

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.

Synonyms
  • Patiromer
  • Patiromer FOS
External IDs
RLY5016
Product Ingredients
IngredientUNIICASInChI Key
Patiromer sorbitex calcium0LB9J2797DNot AvailableNot applicable
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
VeltassaPowder, for suspension8.4 g/1OralRelypsa, Inc.2015-10-23Not applicableUs
VeltassaPowder, for suspension25.2 g/1OralRelypsa, Inc.2015-10-23Not applicableUs
VeltassaPowder, for suspension16.8 g/1OralRelypsa, Inc.2015-10-23Not applicableUs
Categories
UNII
1FQ2RY5YHH
CAS number
1260643-52-4
Weight
Not Available
Chemical Formula
Not Available
InChI Key
Not Available
InChI
Not Available
IUPAC Name
Not Available
SMILES
Not Available

Pharmacology

Indication

For the treatment of hyperkalemia.

Associated Conditions
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
Human
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
Toxicity
Not Available
Affected organisms
  • Humans and other mammals
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
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.
Technetium Tc-99m ciprofloxacinPatiromer can cause a decrease in the absorption of Technetium Tc-99m ciprofloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.
Food Interactions
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]
External Links
KEGG Drug
D10148
PubChem Substance
347910426
ChEMBL
CHEMBL2107875
Wikipedia
Patiromer
FDA label
Download (352 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
2Active Not RecruitingTreatmentHyperkalemia / Resistant Hypertension1
2CompletedPreventionHeart Failure, Unspecified1
2CompletedPreventionHeart Failure, Unspecified / Hyperkalemia1
2CompletedTreatmentChronic Kidney Disease (CKD) / High Blood Pressure (Hypertension) / Hyperkalemia1
2RecruitingTreatmentEnd Stage Renal Disease (ESRD) / ESRD / Hyperkalemia1
2RecruitingTreatmentHyperkalemia1
2TerminatedTreatmentHyperkalemia1
3CompletedTreatmentChronic Kidney Disease (CKD) / Hyperkalemia (HK)1
4CompletedTreatmentChronic Renal Failure (CRF)1
4CompletedTreatmentHyperkalemia1
4RecruitingTreatmentHyperkalemia / Transplant, Kidney1
4RecruitingTreatmentHyperkalemia / Type2 Diabetes1
Not AvailableCompletedTreatmentAcute Decompensated Heart Failure (ADHF)1
Not AvailableRecruitingTreatmentChronic Kidney Disease (CKD) / Hyperkalemia1

Pharmacoeconomics

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

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

Taxonomy

Classification
Not classified

Targets

Kind
Small molecule
Organism
Human
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 09:43 / Updated on December 14, 2018 16:58