Lanthanum carbonate
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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 marketed under the trade name Fosrenol by Shire Pharmaceuticals. It is a large pill that requires thorough chewing to avoid choking and other gastrointestinal adverse effects. It is used to treat elevated phosphate levels, primarily in patients with chronic kidney disease, by binding to dietary phosphate and preventing its absorption in the intestine.2
- 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
Lanthanum carbonate is indicated to reduce serum phosphate in patients with end-stage renal disease (ESRD).2
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Indication Type Indication Combined Product Details Approval Level Age Group Patient Characteristics Dose Form Treatment of Hyperphosphatemia •••••••••••• - 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.2 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.2
In comparison to [sevelemer], another common phosphate binder, lanthanum carbonate is more efficacious in lowering serum phosphate concentrations and effectively managing hyperphosphatemia.1
- 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.2 Both serum phosphate and calcium phosphate product are reduced as a consequence of the reduced dietary phosphate absorption.
Target Actions Organism APhosphate binderHumans - Absorption
The bioavailability of lanthanum carbonate following oral administration is exceedingly low (<0.002%), with a mean Cmax of 1.0 ng/mL and average serum concentration of 0.6 ng/mL.2 The timing of food intake relative to lanthanum administration (during and 30 minutes after food intake) has a negligible effect on the systemic level of lanthanum.2
- 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.2
- Metabolism
Lanthanum does not undergo metabolism.2
- 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.2 Biliary excretion is the predominant route of elimination for circulating lanthanum in rats.2
- Half-life
The elimination half-life of lanthanum in patients undergoing dialysis was 53 hours following discontinuation of therapy.2
- Clearance
In healthy volunteers administered intravenous lanthanum as the soluble chloride salt (120 μg), renal clearance was less than 2% of total plasma clearance.2
- 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.
Drug Interaction Integrate drug-drug
interactions in your softwareAmpicillin The serum concentration of Ampicillin can be decreased when it is combined with Lanthanum carbonate. Atorvastatin The absorption of Atorvastatin can be decreased when combined with Lanthanum carbonate. Benazepril Lanthanum carbonate can cause a decrease in the absorption of Benazepril resulting in a reduced serum concentration and potentially a decrease in efficacy. Captopril Lanthanum carbonate can cause a decrease in the absorption of Captopril resulting in a reduced serum concentration and potentially a decrease in efficacy. Cerivastatin The absorption of Cerivastatin can be decreased when combined with Lanthanum carbonate. - Food Interactions
- Take with food.
Products
- Drug product information from 10+ global regionsOur datasets provide approved product information including:dosage, form, labeller, route of administration, and marketing period.Access drug product information from over 10 global regions.
- Product Ingredients
Ingredient UNII CAS InChI Key Lanthanum carbonate hydrate 490D9F069T 54451-24-0 PKOQIYFBOVTYOH-UHFFFAOYSA-H - Active Moieties
Name Kind UNII CAS InChI Key Lanthanum III cation ionic O7FU5X12W5 16096-89-2 CZMAIROVPAYCMU-UHFFFAOYSA-N - International/Other Brands
- Foznol / Phosbloc
- Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Fosrenol Powder 1000 mg/1 Oral Takeda Pharmaceuticals America, Inc. 2014-09-24 Not applicable US Fosrenol Tablet, chewable 750 mg/1 Oral Takeda Pharmaceuticals America, Inc. 2005-11-23 Not applicable US Fosrenol Tablet, chewable 500 mg/1 Oral Takeda Pharmaceuticals America, Inc. 2004-10-26 Not applicable US Fosrenol Tablet, chewable 1000 mg Oral Takeda 2006-12-06 2024-07-31 Canada Fosrenol Tablet, chewable 500 mg/1 Oral Avera McKennan Hospital 2015-03-03 2017-05-24 US - Generic Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Lanthanum carbonate Tablet, chewable 750 mg/1 Oral Teva Pharmaceuticals USA, Inc. 2022-05-25 Not applicable US Lanthanum carbonate Tablet, chewable 750 mg/1 Oral Cipla USA Inc. 2022-01-25 Not applicable US Lanthanum carbonate Tablet, chewable 500 mg/1 Oral Prasco Laboratories 2017-08-30 Not applicable US Lanthanum Carbonate Tablet, chewable 1000 mg/1 Oral Lupin Pharmaceuticals, Inc. 2017-08-30 Not applicable US Lanthanum carbonate Tablet, chewable 750 mg/1 Oral Exelan Pharmaceuticals, Inc. 2022-01-25 Not applicable US
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
- Nain P, Nayak N, Maj MC, Singh RK, Kaur J, Jeong Y, Maity S, Nath R, Hilgers RH, Nauhria S, Nauhria S: Efficacy of Lanthanum Carbonate and Sevelamer Carbonate as Phosphate Binders in Chronic Kidney Disease-A Comparative Clinical Study. Pharmacy (Basel). 2023 Feb 2;11(1):27. doi: 10.3390/pharmacy11010027. [Article]
- FDA Approved Drug Products: Fosrenol (lanthanum carbonate) chewable tablets/oral powder for oral use (December 2023) [Link]
- External Links
- PubChem Compound
- 168924
- PubChem Substance
- 310264888
- ChemSpider
- 147758
- 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
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 Phase Status Purpose Conditions Count Start Date Why Stopped 100+ additional columns Unlock 175K+ rows when you subscribe.View sample dataNot Available Completed Not Available Chronic Kidney Disease (CKD) 1 somestatus stop reason just information to hide Not Available Completed Not Available End Stage Renal Disease (ESRD) 1 somestatus stop reason just information to hide Not Available Completed Not Available Hyperphosphataemia 3 somestatus stop reason just information to hide Not Available Completed Not Available Hyperphosphataemia / Kidney Diseases 1 somestatus stop reason just information to hide Not Available Completed Prevention Chronic Kidney Disease (CKD) 2 somestatus stop reason just information to hide
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Not Available
- Dosage Forms
Form Route Strength Powder Oral Powder Oral 500 mg Powder Oral 1000 mg/1 Powder Oral 750 mg/1 Tablet, chewable Oral Tablet, chewable Oral 250 mg/1 Tablet, chewable Oral 500 mg/1 Tablet, chewable Oral 954 MG Tablet, chewable Oral 500 mg Tablet, chewable Oral 750 mg Powder Oral 1000 MG Powder Oral 750 MG Tablet, chewable Oral 1000 MG Tablet, chewable Oral 250 MG Tablet, chewable Oral 1000 mg/1 Tablet, chewable Oral 750 mg/1 - Prices
- Not Available
- Patents
Patent Number Pediatric Extension Approved Expires (estimated) Region US5968976 No 1999-10-19 2018-10-26 US US7381428 No 2008-06-03 2024-08-26 US US7465465 No 2008-12-16 2024-08-26 US US8980327 No 2015-03-17 2030-12-01 US US9023397 No 2015-05-05 2030-12-01 US
Properties
- State
- Solid
- Experimental Properties
Property Value Source water solubility Practically insoluble. FDA Label - Predicted Properties
Property Value Source Water Solubility 31.0 mg/mL ALOGPS logP 0.65 ALOGPS logP 0.25 Chemaxon logS -1.2 ALOGPS pKa (Strongest Acidic) 6.05 Chemaxon Physiological Charge -1 Chemaxon Hydrogen Acceptor Count 3 Chemaxon Hydrogen Donor Count 0 Chemaxon Polar Surface Area 63.19 Å2 Chemaxon Rotatable Bond Count 0 Chemaxon Refractivity 31.17 m3·mol-1 Chemaxon Polarizability 3.52 Å3 Chemaxon Number of Rings 0 Chemaxon Bioavailability 1 Chemaxon Rule of Five Yes Chemaxon Ghose Filter No Chemaxon Veber's Rule No Chemaxon MDDR-like Rule No Chemaxon - Predicted ADMET Features
- Not Available
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
- Not Available
- Chromatographic Properties
Collision Cross Sections (CCS)
Not Available
Targets
Drug created at September 14, 2010 16:21 / Updated at October 03, 2024 07:20