Petadeferitrin

CAS911714-45-9

MFC16H21NO6S MW355.4 g/mol

(4S)-2-[2-hydroxy-4-[2-(2-methoxyethoxy)ethoxy]phenyl]-4-methyl-5H-1,3-thiazole-4-carboxylic acid

• (4S)-4,5-Dihydro-2-(2-hydroxy-4-(2-(2-methoxyethoxy)ethoxy)phenyl)-4-methyl-4-thiazolecarboxylic acid
• 4-Thiazolecarboxylic acid, 4,5-dihydro-2-(2-hydroxy-4-(2-(2-methoxyethoxy)ethoxy)phenyl)-4-methyl-, (4S)-
• (4S)-4,5-dihydro-2-[2-hydroxy-4-[2-(2-methoxyethoxy)ethoxy]phenyl]-4-methyl-4-thiazolecarboxylic acid

(4S)-2-{2-hydroxy-4-[2-(2-methoxyethoxy)ethoxy]phenyl}-4-methyl4,5-dihydro-1,3-thiazole-4-carboxylic acid
iron chelating agent, SP 420, WBX54NZ436

Petadeferitrin is an orally bioavailable iron-chelating agent and derivative of desferrithiocin, with iron chelating and protective activities in diseases of iron overload. Upon oral administration, petadeferitrin targets, binds to and chelates free iron. This induces the excretion of iron, prevents iron accumulation and prevents cellular and/or tissue damage associated with iron overload.

Petadeferitrin (formerly known as SP-420) is an investigational, orally bioavailable, small-molecule iron chelator being developed by Pharmacosmos (and its subsidiary Abfero Pharmaceuticals) to treat patients with transfusion-dependent iron overload. The drug works by binding to excess free iron in the body and forming complexes that are primarily excreted through bile and feces.

Key Characteristics & Mechanisms

• Drug Class: It is a tridentate iron chelator and a derivative of desferrithiocin.
• Enhanced Efficiency: In preclinical studies, it demonstrated a higher iron clearance efficiency (ICE value of 26.7) compared to desferrithiocin.
• Brain-Penetrant: It is uniquely characterized as a brain-penetrant agent, which could expand its potential protective use in specific diseases associated with iron accumulation.

Clinical Development Status

• Investigational Status: The drug remains investigational and has not yet been approved for commercial use anywhere in the world.
• Target Diseases: Clinical evaluation focuses on individuals who suffer from iron overload due to frequent blood transfusions, such as patients with β-thalassemia and sickle cell disease.
• Ongoing Studies: Pharmacosmos is actively evaluating the drug in Phase II clinical trials (such as ClinicalTrials.gov ID NCT05693909) to assess its safety, tolerability, and dosing advantages over existing options. Early human data suggests it may offer effective clearance with less frequent dosing compared to some currently approved alternatives.

• A Trial Testing SP-420 in Subjects With Transfusion-dependent β-thalassemia or Low-risk Myelodysplastic SyndromesCTID:NCT05693909Phase:Phase 2Status:RecruitingDate:2025-09-24
• Safety of SP-420 in the Treatment of Transfusional Iron OverloadCTID:NCT04741542Phase:Phase 1Status:TerminatedDate:2024-12-27
• SP-420 in Subjects With Transfusion-dependent Beta-Thalassemia or Other Rare AnemiasCTID:NCT03801889Phase:Phase 2Status:WithdrawnDate:2020-10-05
• Safety and Pharmacokinetic Study of Escalating Doses of SP-420, an Iron Chelator, in Patients With β-ThalassemiaCTID:NCT02274233Phase:Phase 1Status:TerminatedDate:2015-09-29

An open-label, dose-escalation, dose-finding, and proof-of-concept trial of SP-420 in subjects with transfusion-dependent β-thalassemiaEudraCT:2022-002395-36

Phase:Phase 2, Status:Trial now transitioned, Date:2022-12-16

SYN

https://patentscope.wipo.int/search/en/detail.jsf?docId=US42268401&_cid=P21-MSCM3W-69668-1

SYN

https://patentscope.wipo.int/search/en/detail.jsf?docId=WO2006107626&_cid=P21-MSCM3W-69668-1

PAT

https://patentscope.wipo.int/search/en/detail.jsf?docId=US43268075&_cid=P21-MSCM3W-69668-1

PAT

Desferrithiocin polyether analoguesPublication Number:

US-2017217912-A1Priority Date:

2005-04-04

• Deferithiocin polyether analoguePublication Number:JP-6178816-B2Priority Date:2005-04-04Grant Date:2017-08-09
• Deferithiocin polyether analoguePublication Number:JP-2008536833-APriority Date:2005-04-04
• Desferrithiocin polyether analoguesPublication Number:EP-3190106-A1Priority Date:2005-04-04
• Desferrithiocin polyether analoguesPublication Number:US-9567309-B2Priority Date:2005-04-04Grant Date:2017-02-14
• Desferrithiocin polyether analoguesPublication Number:US-2013030028-A1Priority Date:2005-04-04

ADVERTISEMENT

ANAX LABORATORIES

WEBSITE https://www.anaxlab.com/

Discovery Solutions, Supporting the chemistry needs of clients in the Medical, Analytical and Bio Sciences

Development Solutions, Developing from Lab scale to PR&D, Kilo Scale-ups and Commercial Scales

SEE MORE………Integrated Solutions, Manufacturing Solutions, Products,
Can’t Find? Let’s Connect

Phone : +91 897704 2010 /  +91 9177075735, Email : info@anaxlab.com

#MedicinalChemistry, #DrugDiscovery, #OrganicSynthesis, #ChemicalLibrary, #BuildingBlocks, #SARStudies, #ChemistryInnovation, #medchem, #Drugdevelopment, #Biotech, #Biotechnology, #AnaxLaboratories, #Pharma

AS ON FEB2026 4.574 LAKHS VIEWS ON BLOG WORLDREACH AVAILABLEFOR YOUR ADVERTISEMENT

join me on Linkedin

Anthony Melvin Crasto Ph.D – India | LinkedIn

join me on Researchgate

RESEARCHGATE

join me on Facebook

Anthony Melvin Crasto Dr. | Facebook

• Twitter
• FACEBOOK

join me on twitter

Anthony Melvin Crasto Dr. | twitter

+919321316780 call whatsaapp

EMAIL. amcrasto@gmail.com

References

• Target Class Profiling of Small-Molecule MethyltransferasesPublication Name:ACS Chemical BiologyPublication Date:2023-03-28PMCID:PMC10983791PMID:36976909DOI:10.1021/acschembio.3c00124
• Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitorsPublication Name:Proceedings of the National Academy of Sciences of the United States of AmericaPublication Date:2020-11-23PMCID:PMC7733812PMID:33229545DOI:10.1073/pnas.2005463117
• Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput ScreeningPublication Name:SLAS discovery : advancing life sciences R & DPublication Date:2020-01PMCID:PMC10791069PMID:31498718DOI:10.1177/2472555219873068
• A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoproteinPublication Name:Molecular PharmacologyPublication Date:2019-11PMCID:PMC6790066PMID:31515284DOI:10.1124/mol.119.115964
• Safety and pharmacokinetics of the oral iron chelator SP‐420 in β‐thalassemiaPublication Name:American Journal of HematologyPublication Date:2017-10-31PMID:28940308DOI:10.1002/ajh.24914
• Metabolically programmed iron chelatorsPublication Name:Bioorganic & Medicinal ChemistryPublication Date:2015-09-01PMCID:PMC4608554PMID:26231739DOI:10.1016/j.bmc.2015.06.059
• Substituent Effects on Desferrithiocin and Desferrithiocin Analogue Iron-Clearing and Toxicity ProfilesPublication Name:Journal of Medicinal ChemistryPublication Date:2012-08-13PMCID:PMC3583384PMID:22889170DOI:10.1021/jm300509y
• CCDC 757291: Experimental Crystal Structure DeterminationPublication Date:2011DOI:10.5517/cctf0rz
• The Impact of Polyether Chain Length on the Iron Clearing Efficiency and Physiochemical Properties of Desferrithiocin AnaloguesPublication Name:Journal of Medicinal ChemistryPublication Date:2010-04-08PMCID:PMC2951135PMID:20232803DOI:10.1021/jm9018146

/////////petadeferitrin, ANAX LABS, iron chelating agent, SP 420, WBX54NZ436

#petadeferitrin, #ANAX LABS, #iron chelating agent, #SP 420, #WBX54NZ436