Identification

Summary

Lanthanum carbonate is a phosphate binder indicated for the reduction of serum phosphate in patients with end stage renal disease.

Brand Names
Fosrenol
Generic Name
Lanthanum carbonate
DrugBank Accession Number
DB06792
Background

Lanthanum carbonate is a phosphate binder commonly used in clinical practice. It is marketed under the trade name Fosrenol by Shire Pharmaceuticals. It is the largest of all pills filled in community pharmacies. Sometimes patients forget that Fosrenol is not swallowed whole, but instead should be chewed. This has led to severe choking. It is prescribed for treating high phosphate levels, mainly found in patients with chronic kidney disease. Lanthanum should be taken with meals and binds to phosphate in the diet, preventing phosphate absorption in the intestine.

Type
Small Molecule
Groups
Approved
Structure
Weight
Average: 457.835
Monoisotopic: 457.76695
Chemical Formula
C3La2O9
Synonyms
  • Lanthanum (III) carbonate
  • Lanthanum carbonate anhydrous
  • Lanthanum sesquicarbonate
  • Lanthanum(3+) carbonate

Pharmacology

Indication

Used to reduce serum phosphate in patients with end stage renal disease (ESRD).

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Associated Conditions
Contraindications & Blackbox Warnings
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Pharmacodynamics

In vitro studies have shown that lanthanum binds phosphate in the physiologically relevant pH range of 3 to 7. In simulated gastric fluid, lanthanum binds approximately 97% of the available phosphate at pH 3-5 and 67% at pH 7, when lanthanum is present in a two-fold molar excess to phosphate. Bile acids have not been shown to affect the phosphate binding affinity of lanthanum. In order to bind dietary phosphate, lanthanum carbonate must be administered with or immediately after meals.

Mechanism of action

Lanthanum carbonate is a phosphate binder that reduces absorption of phosphate by forming insoluble lanthanum phosphate complexes that pass through the gastrointestinal (GI) tract unabsorbed. Both serum phosphate and calcium phosphate product are reduced as a consequence of the reduced dietary phosphate absorption.

TargetActionsOrganism
APhosphate
binder
Humans
Absorption

Bioavailability very low (<0.002%) following single or multiple dose oral administration.

Volume of distribution

Not Available

Protein binding

In vitro, lanthanum is highly bound (>99%) to human plasma proteins, including human serum albumin, α1-acid glycoprotein, and transferrin.

Metabolism

Lanthanum is not metabolized.

Route of elimination

No information is available regarding the mass balance of lanthanum in humans after oral administration. In rats and dogs, the mean recovery of lanthanum after an oral dose was about 99% and 94%, respectively, and was essentially all from feces. Biliary excretion is the predominant route of elimination for circulating lanthanum in rats.

Half-life

Elimination half-life of 53 hours.

Clearance

In healthy volunteers administered intravenous lanthanum as the soluble chloride salt (120 μg), renal clearance was less than 2% of total plasma clearance.

Adverse Effects
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Toxicity

The symptoms associated with overdose are adverse reactions such as headache, nausea and vomiting. Lanthanum carbonate was not acutely toxic in animals by the oral route. No deaths and no adverse effects occurred in mice, rats or dogs after single oral doses of 2000 mg/kg.

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
AmpicillinThe serum concentration of Ampicillin can be decreased when it is combined with Lanthanum carbonate.
AtorvastatinThe absorption of Atorvastatin can be decreased when combined with Lanthanum carbonate.
BenazeprilLanthanum carbonate can cause a decrease in the absorption of Benazepril resulting in a reduced serum concentration and potentially a decrease in efficacy.
CaptoprilLanthanum carbonate can cause a decrease in the absorption of Captopril resulting in a reduced serum concentration and potentially a decrease in efficacy.
CerivastatinThe absorption of Cerivastatin can be decreased when combined with Lanthanum carbonate.
ChloroquineLanthanum carbonate can cause a decrease in the absorption of Chloroquine resulting in a reduced serum concentration and potentially a decrease in efficacy.
CilazaprilLanthanum carbonate can cause a decrease in the absorption of Cilazapril resulting in a reduced serum concentration and potentially a decrease in efficacy.
CinoxacinLanthanum carbonate can cause a decrease in the absorption of Cinoxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.
CiprofloxacinLanthanum carbonate can cause a decrease in the absorption of Ciprofloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.
DelafloxacinLanthanum carbonate can cause a decrease in the absorption of Delafloxacin resulting in a reduced serum concentration and potentially a decrease in efficacy.
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Food Interactions
  • Take with food.

Products

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Product Ingredients
IngredientUNIICASInChI Key
Lanthanum carbonate hydrate490D9F069T54451-24-0PKOQIYFBOVTYOH-UHFFFAOYSA-H
Active Moieties
NameKindUNIICASInChI Key
Lanthanum III cationionicO7FU5X12W516096-89-2CZMAIROVPAYCMU-UHFFFAOYSA-N
International/Other Brands
Foznol / Phosbloc
Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
FosrenolTablet, chewable1000 mg/1OralTakeda Pharmaceuticals America, Inc.2005-11-23Not applicableUS flag
FosrenolTablet, chewable500 mg/1OralShire2004-10-262008-05-31US flag
FosrenolTablet, chewable250 mgOralTakeda2006-12-06Not applicableCanada flag
FosrenolTablet, chewable750 mgOralTakeda2006-12-06Not applicableCanada flag
FosrenolPowder1000 mg/1OralTakeda Pharmaceuticals America, Inc.2014-09-24Not applicableUS flag
FosrenolTablet, chewable750 mg/1OralTakeda Pharmaceuticals America, Inc.2005-11-23Not applicableUS flag
FosrenolTablet, chewable250 mg/1OralShire2004-10-262008-01-31US flag
FosrenolTablet, chewable1000 mgOralTakeda2006-12-06Not applicableCanada flag
FosrenolTablet, chewable500 mg/1OralAvera McKennan Hospital2015-03-032017-05-24US flag
FosrenolPowder750 mg/1OralTakeda Pharmaceuticals America, Inc.2014-09-24Not applicableUS flag
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
Lanthanum carbonateTablet, chewable750 mg/1OralPrasco Laboratories2017-08-30Not applicableUS flag
Lanthanum carbonateTablet, chewable1000 mg/1OralCipla USA Inc.2022-01-25Not applicableUS flag
Lanthanum CarbonateTablet, chewable750 mg/1OralLupin Pharmaceuticals, Inc.2017-08-30Not applicableUS flag
Lanthanum carbonateTablet, chewable1000 mg/1OralExelan Pharmaceuticals, Inc.2022-01-25Not applicableUS flag
Lanthanum carbonateTablet, chewable500 mg/1OralPrasco Laboratories2017-08-30Not applicableUS flag
Lanthanum carbonateTablet, chewable750 mg/1OralTeva Pharmaceuticals USA, Inc.2022-05-25Not applicableUS flag
Lanthanum carbonateTablet, chewable750 mg/1OralCipla USA Inc.2022-01-25Not applicableUS flag
Lanthanum CarbonateTablet, chewable500 mg/1OralLupin Pharmaceuticals, Inc.2017-08-30Not applicableUS flag
Lanthanum carbonateTablet, chewable750 mg/1OralExelan Pharmaceuticals, Inc.2022-01-25Not applicableUS flag
Lanthanum carbonateTablet, chewable1000 mg/1OralPrasco Laboratories2017-08-30Not applicableUS flag

Categories

ATC Codes
V03AE03 — Lanthanum carbonate
Drug Categories
Chemical TaxonomyProvided by Classyfire
Description
This compound belongs to the class of organic compounds known as organic carbonic acids. These are compounds comprising the carbonic acid functional group.
Kingdom
Organic compounds
Super Class
Organic acids and derivatives
Class
Organic carbonic acids and derivatives
Sub Class
Organic carbonic acids
Direct Parent
Organic carbonic acids
Alternative Parents
Carbonate salts / Organic salts / Organic oxides / Hydrocarbon derivatives / Carbonyl compounds
Substituents
Aliphatic acyclic compound / Carbonate salt / Carbonic acid / Carbonyl group / Hydrocarbon derivative / Organic oxide / Organic oxygen compound / Organic salt / Organooxygen compound
Molecular Framework
Not Available
External Descriptors
Not Available
Affected organisms
  • Humans and other mammals

Chemical Identifiers

UNII
0M78EU4V9H
CAS number
587-26-8
InChI Key
NZPIUJUFIFZSPW-UHFFFAOYSA-H
InChI
InChI=1S/3CH2O3.2La/c3*2-1(3)4;;/h3*(H2,2,3,4);;/q;;;2*+3/p-6
IUPAC Name
dilanthanum(3+) ion tricarbonate
SMILES
[La+3].[La+3].[O-]C([O-])=O.[O-]C([O-])=O.[O-]C([O-])=O

References

General References
Not Available
PubChem Compound
168924
PubChem Substance
310264888
ChemSpider
147758
RxNav
1311070
ChEMBL
CHEMBL2096647
Drugs.com
Drugs.com Drug Page
Wikipedia
Lanthanum_carbonate
FDA label
Download (311 KB)
MSDS
Download (122 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
4Active Not RecruitingTreatmentCardiovascular Disease (CVD) / Chronic Kidney Disease (CKD)1
4CompletedTreatmentChronic Kidney Disease (CKD)1
4CompletedTreatmentRenal Failure, Chronic Renal Failure1
4Enrolling by InvitationTreatmentHyperphosphataemia / Metabolic Bone Disorder / Renal Insufficiency,Chronic1
4RecruitingOtherVariola Major (Smallpox)1
4TerminatedTreatmentKidney Diseases1
4Unknown StatusTreatmentOther Nonspecific Abnormal Serum Enzyme Levels1
3CompletedTreatmentChronic Kidney Disease (CKD) / Impaired Renal Function / Renal Dialysis1
3CompletedTreatmentHemodialysis Treatment / Hyperphosphataemia1
3CompletedTreatmentHyperphosphataemia4

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage Forms
FormRouteStrength
PowderOral1000 mg/1
PowderOral750 mg/1
Tablet, chewableOral250 mg/1
Tablet, chewableOral500 mg/1
Tablet, chewableOral
PowderOral
Tablet, chewableOral500 mg
Tablet, chewableOral750 mg
PowderOral1000 MG
PowderOral750 MG
Tablet, chewableOral1000 MG
Tablet, chewableOral250 MG
Tablet, chewableOral1000 mg/1
Tablet, chewableOral750 mg/1
Prices
Not Available
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)Region
US5968976No1999-10-192018-10-26US flag
US7381428No2008-06-032024-08-26US flag
US7465465No2008-12-162024-08-26US flag
US8980327No2015-03-172030-12-01US flag
US9023397No2015-05-052030-12-01US flag

Properties

State
Solid
Experimental Properties
PropertyValueSource
water solubilityPractically insoluble.FDA Label
Predicted Properties
PropertyValueSource
Water Solubility31.0 mg/mLALOGPS
logP0.65ALOGPS
logP0.25ChemAxon
logS-1.2ALOGPS
pKa (Strongest Acidic)6.05ChemAxon
Physiological Charge-1ChemAxon
Hydrogen Acceptor Count3ChemAxon
Hydrogen Donor Count0ChemAxon
Polar Surface Area63.19 Å2ChemAxon
Rotatable Bond Count0ChemAxon
Refractivity31.17 m3·mol-1ChemAxon
Polarizability3.52 Å3ChemAxon
Number of Rings0ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterNoChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleNoChemAxon
Predicted ADMET Features
Not Available

Spectra

Mass Spec (NIST)
Not Available
Spectra
Not Available

Targets

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Kind
Small molecule
Organism
Humans
Pharmacological action
Yes
Actions
Binder
References
  1. Behets GJ, Verberckmoes SC, D'Haese PC, De Broe ME: Lanthanum carbonate: a new phosphate binder. Curr Opin Nephrol Hypertens. 2004 Jul;13(4):403-9. [Article]

Drug created at September 14, 2010 16:21 / Updated at August 19, 2022 08:38