Cambritaxestat

CAS 1979939-16-6

MFC25H22ClF3N4O2 MW502.9 g/mol

N-[(1S)-1-(4-chlorophenyl)ethyl]-3-[3-[[4-(trifluoromethoxy)phenyl]methyl]imidazo[4,5-b]pyridin-2-yl]propanamide

N-[(1S)-1-(4-chlorophenyl)ethyl]-3-(3-{[4-(trifluoromethoxy)phenyl]methyl}-3H-imidazo[4,5-b]pyridin-2-yl)propanamide
autotaxin inhibitor, antineoplastic, Orphan Drug, IOA 289, IOA-289, IOA289, LYY3P2KA27, CRT 0273750

• OriginatorCancer Research Technology; Merck & Co
• DeveloperiOnctura
• ClassAntifibrotics; Antineoplastics; Small molecules
• Mechanism of ActionAngiogenesis inhibitors; Cell proliferation inhibitors; ENPP2 protein inhibitors
• Orphan Drug StatusYes – Pancreatic cancer
• Phase I/IIPancreatic cancer
• Phase ISolid tumours
• PreclinicalNon-alcoholic steatohepatitis
• 14 Oct 2025Efficacy and adverse event data from a phase I/II trial in Pancreatic cancer released by iOnctura
• 04 Oct 2024Cambritaxestat is still in phase-I development in Solid-tumours (In volunteers) in Italy (PO, Capsule) (NCT05027568)
• 31 May 2024Efficacy and adverse event data from a phase I/II trial in Pancreatic cancer presented at the 60th Annual Meeting of the American Society of Clinical Oncology (ASCO-2024)

Cambritaxestat is an autotaxin inhibitor.

Cambritaxestat is an orally bioavailable small molecule inhibitor of autotaxin (ATX; ectonucleotide pyrophosphatase/phosphodiesterase family member 2; ENPP2), with potential antifibrotic and antineoplastic activities. Upon oral administration, cambritaxestat targets and binds to both the substrate pocket and the lysophosphatidic acid (LPA) carrier channel of ATX, thereby inhibiting the activity of ATX. This both directly inhibits the proliferation of tumor cells and reduces fibrosis in the tumor microenvironment (TME), allowing lymphocytes to infiltrate into the tumor and enhancing immune responses against tumor cells. ATX, a secreted glycoprotein with lysophospholipase D activity, hydrolyzes lysophosphatidylcholine (LPC) to LPA. LPA-mediated signaling plays an important role in cellular migration, proliferation and survival in fibrotic response. ATX and LPA are overexpressed in many tumors.

• A Study to Assess an ATX Inhibitor (IOA-289) in Healthy VolunteersCTID: NCT05027568Phase: Phase 1Status: CompletedDate: 2025-03-20
• A Study to Assess an ATX Inhibitor (IOA-289) in Patients with Metastatic Pancreatic CancerCTID: NCT05586516Phase: Phase 1/Phase 2Status: Active, not recruitingDate: 2025-03-20

SYN

WO2016/124939

https://patentscope.wipo.int/search/en/detail.jsf?docId=WO2016124939&_cid=P22-MKBYYZ-98558-1

SYN

https://patentscope.wipo.int/search/en/detail.jsf;jsessionid=D2AB83A7D50F3F6B36DBA4001867C8E7.wapp2nC?docId=WO2024246264&_cid=P22-MKBYUT-93851-1

WO2016/124939 describes various ATX inhibitor compounds and their use in the treatment of proliferative disorders in which ATX activity is implicated, including Compound 1.

Compound 1 is example 40 in WO2016/124939, which document is incorporated herein by reference in its entirety. WO2016/124939 describes over 200 examples. Compound 1’s structure is according to Formula I.

PAT

• Autotaxin inhibitory compoundsPublication Number: US-10654846-B2Priority Date: 2015-02-06Grant Date: 2020-05-19
• Autotaxin inhibitory compoundsPublication Number: EP-3253737-B3Priority Date: 2015-02-06Grant Date: 2024-05-29
• Autotaxin inhibitor compoundsPublication Number: ES-2778898-T7Priority Date: 2015-02-06Grant Date: 2024-11-15
• Autotaxin inhibitory compoundsPublication Number: EP-3253737-A1Priority Date: 2015-02-06
• Home chemokine inhibiting compoundsPublication Number: CN-107428752-BPriority Date: 2015-02-06Grant Date: 2021-06-29
• Autotaxin inhibitory compoundsPublication Number: US-11453666-B2Priority Date: 2015-02-06Grant Date: 2022-09-27
• Autotaxin Inhibitory CompundsPublication Number: US-2020283435-A1Priority Date: 2015-02-06
• Autotaxin inhibitory compoundsPublication Number: WO-2016124939-A1Priority Date: 2015-02-06
• A pi3k-delta inhibitor for the treatment of pancreatic cancerPublication Number: WO-2022207648-A1Priority Date: 2021-03-29
• A pi3k-delta inhibitor for the treatment of pancreatic cancerPublication Number: EP-4313059-A1Priority Date: 2021-03-29
• A pi3k-delta inhibitor for the treatment of pancreatic cancerPublication Number: US-2024216385-A1Priority Date: 2021-03-29
• Autotaxin inhibitory compoundsPublication Number: EP-3253737-B1Priority Date: 2015-02-06Grant Date: 2020-01-08
• Autotaxin inhibitory compoundsPublication Number: US-2018016274-A1Priority Date: 2015-02-06
• Autotaxin (atx) inhibitor for the treatment of pancreatic cancerPublication Number: WO-2022258693-A1Priority Date: 2021-06-09
• Autotaxin (atx) inhibitor for the treatment of pancreatic cancerPublication Number: US-2025057820-A1Priority Date: 2021-06-09
• Autotaxin (atx) inhibitor for the treatment of pancreatic cancerPublication Number: EP-4351563-A1Priority Date: 2021-06-09
• Autotaxin (ATX) inhibitors for the treatment of pancreatic cancerPublication Number: CN-117295496-APriority Date: 2021-06-09
• PI3K-δ inhibitors for the treatment of pancreatic cancerPublication Number: CN-116997340-APriority Date: 2021-03-29

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• Characterization and translational development of IOA-289, a novel autotaxin inhibitor for the treatment of solid tumorsPublication Name: Immuno-Oncology and TechnologyPublication Date: 2023-06PMCID: PMC10205783PMID: 37234285DOI: 10.1016/j.iotech.2023.100384
• The IUPHAR Guide to Immunopharmacology: connecting immunology and pharmacologyPublication Name: ImmunologyPublication Date: 2020-03-02PMCID: PMC7160657PMID: 32020584DOI: 10.1111/imm.13175
• Discovery of potent inhibitors of the lysophospholipase autotaxinPublication Name: Bioorganic & Medicinal Chemistry LettersPublication Date: 2016-11-15PMID: 27780639DOI: 10.1016/j.bmcl.2016.10.036

///////Cambritaxestat, autotaxin inhibitor, antineoplastic, Orphan Drug, IOA 289, IOA-289, IOA289, LYY3P2KA27, CRT 0273750