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Asundexian
Asundexian
CAS 2064121-65-7
MW 592.9 g/mol, C26H21ClF4N6O4
4-[[(2S)-2-[4-[5-chloro-2-[4-(trifluoromethyl)triazol-1-yl]phenyl]-5-methoxy-2-oxo-1-pyridinyl]butanoyl]amino]-2-fluorobenzamide
- (S)-4-(2-(4-(5-Chloro-2-(4-(trifluoromethyl)-1H-1,2,3-triazol-1-yl)phenyl)-5-methoxy-2-oxopyridin-1(2H)-yl)butanamido)-2-fluorobenzamide
- 4-[[(2~{S})-2-[4-[5-chloranyl-2-[4-(trifluoromethyl)-1,2,3-triazol-1-yl]phenyl]-5-methoxy-2-oxidanylidene-pyridin-1-yl]butanoyl]amino]-2-fluoranyl-benzamide
- (S)-4-[2-[4-[5-Chloro-2-[4-(trifluoromethyl)-1H-1,2,3-triazol-1-yl]phenyl]-5-methoxy-2-oxopyridin-1(2H)-yl]butanamido]-2-fluorobenzamide
APPROVALS 2026, FDA 2026, Sunharbo, LA585UM8DE, BAY2433334, BAY 2433334
To reduce the risk of stroke in adults following a recent mild-to-moderate non-cardioembolic ischemic stroke or a high-risk transient ischemic attack
Asundexian, sold under the brand name Sunharbo, is a Factor XIa inhibitor developed by Bayer to prevent stroke.[1][2]
Clinical trials
Asundexian efficacy and safety in patients have been evaluated in two clinical trial programs: phase IIb PACIFIC and phase III OCEANIC.[3] In the phase IIb PACIFIC clinical trial programs, asundexian consistently showed no difference in bleeding rate compared with placebo[4][5] and reduced the risk of bleeding compared with apixaban.[6] All three trials in the programs were not powered to show efficacy of asundexian.[3] However, a phase III trial, OCEANIC-AF, demonstrated a hazard ratio of 3.8 for stroke or systemic embolism with asundexian vs apixaban, so it was stopped due to a “lack of efficacy.” The remaining active study OCEANIC-STROKE was recommended to continue as planned. Bayer is reevaluating the design of the OCEANIC-AFINA based on the findings of the OCEANIC trial.[7]
In February 2026, the OCEANIC-STROKE trial was completed. This was a multicentre, randomised, double-blind, placebo-controlled study involving 12,000 people worldwide who had suffered a non-cardioembolic ischaemic stroke or a transient ischaemic attack. The trial revealed a 26% reduction in the rate of recurrence without major bleeding, a typical complication of antithrombotic drugs.[8][9][10]
SYN
US20180194745 – Substituted oxopyridine derivatives
Example 235
4-({(2S)-2-[4-{5-Chloro-2-[4-(trifluoromethyl)-1H-1,2,3-triazol-1-yl]phenyl}-5-methoxy-2-oxopyridin-1(2H)-yl]butanoyl}amino)-2-fluorobenzamide (Enantiomer 2)
| Separating method: column: Chiralpak AD-H SFC, 5 μm 250 mm×20 mm; mobile phase: carbon dioxide 75%/ethanol 25%; temperature: 40° C.; flow rate: 80 ml/min; pressure: 100 bar; UV detection: 210 nm. |
| Analysis: column: Daicel AD SFC 3 μm, 100 mm×4.6 mm; mobile phase: 75% carbon dioxide, 25% ethanol; flow rate: 3 ml/min; UV detection: 210 nm. |
SYN1
MEDKOO
Synthetic Reference
Design and Preclinical Characterization Program toward Asundexian (BAY 2433334), an Oral Factor XIa Inhibitor for the Prevention and Treatment of Thromboembolic Disorders
By: Roehrig, Susanne; et al
Journal of Medicinal Chemistry (2023), 66(17), 12203-12224
SYN2
Synthetic Reference
Study on Preparation Process of Anticoagulant BAY2433334
By: Zeng, Yanqun; et al
Molecules (2024), 29(24), 6039
SYN3
Synthetic Reference
Preparation of triazole containing oxopyridine derivative and its application in medicine
Assignee: Tianjin Institute of Pharmaceutical Research Co., Ltd.
Inventors: Wei, Qunchao; et al
China
Patent#CN116903585 A
SYN REF
- Discovery of potent, highly selective, and orally bioavailable factor XIa inhibitors for anticoagulant therapyPublication Name:European Journal of Medicinal ChemistryPublication Date:2025-05-05PMID:40010270DOI:10.1016/j.ejmech.2025.117436
- Discovery of potent and selective factor XIa inhibitors incorporating triazole-based benzoic acid as novel P2’ fragments: Molecular dynamics simulations and anticoagulant activityPublication Name:European Journal of Medicinal ChemistryPublication Date:2025-01-15PMID:39580913DOI:10.1016/j.ejmech.2024.117067
- Design, synthesis and biological evaluation of 6-chloro-quinolin-2-one derivatives as novel FXIa inhibitorsPublication Name:Bioorganic & Medicinal Chemistry LettersPublication Date:2024-02-01PMID:38211702DOI:10.1016/j.bmcl.2024.129610
- Design and Preclinical Characterization Program toward Asundexian (BAY 2433334), an Oral Factor XIa Inhibitor for the Prevention and Treatment of Thromboembolic DisordersPublication Name:Journal of Medicinal ChemistryPublication Date:2023-09-05PMCID:PMC10510402PMID:37669040DOI:10.1021/acs.jmedchem.3c00795
- Factor XIa Inhibitors in Anticoagulation Therapy: Recent Advances and PerspectivesPublication Name:Journal of Medicinal ChemistryPublication Date:2023-04-10PMID:37037122DOI:10.1021/acs.jmedchem.2c02130
Pat
- Process for the preparation of monoazo dyesPublication Number:DE-522201-CPriority Date:1928-05-15Grant Date:1931-04-01, Publication Number:BE-638782-A, Publication Number:BE-625897-A, Publication Number:BE-499305-A
- Synthesis of 13-alkyl-gon-4-onesPublication Number:US-3959322-APriority Date:1960-09-22Grant Date:1976-05-25
- Self-supporting explosives mixture that can be deformed into foils and other structuresPublication Number:DE-1124412-BPriority Date:1960-08-17
- Process for the production of chemical compoundsPublication Number:DE-1445151-A1Priority Date:1959-09-25
- Polyepoxide diphenolic acid amide compositions and said compositions modified with aldehyde condensatesPublication Number:US-2907740-APriority Date:1958-10-14Grant Date:1959-10-06
- Process for the production of alcoholsPublication Number:DE-933864-C
References
- Heitmeier, Stefan; Visser, Mayken; Tersteegen, Adrian; Dietze-Torres, Julia; Glunz, Julia; Gerdes, Christoph; Laux, Volker; Stampfuss, Jan; Roehrig, Susanne (June 2022). “Pharmacological profile of asundexian, a novel, orally bioavailable inhibitor of factor XIa”. Journal of Thrombosis and Haemostasis. 20 (6): 1400–1411. doi:10.1111/jth.15700. PMC 9313898. PMID 35289054.
- Roehrig, Susanne; Ackerstaff, Jens; Jiménez Núñez, Eloísa; Teller, Henrik; Ellerbrock, Pascal; Meier, Katharina; Heitmeier, Stefan; Tersteegen, Adrian; Stampfuss, Jan; Lang, Dieter; Schlemmer, Karl-Heinz; Schaefer, Martina; Gericke, Kersten M.; Kinzel, Tom; Meibom, Daniel (2023-09-05). “Design and Preclinical Characterization Program toward Asundexian (BAY 2433334), an Oral Factor XIa Inhibitor for the Prevention and Treatment of Thromboembolic Disorders”. Journal of Medicinal Chemistry. 66 (17): 12203–12224. doi:10.1021/acs.jmedchem.3c00795. ISSN 0022-2623. PMC 10510402. PMID 37669040.
- “Bayer initiates landmark Phase III study program to investigate oral FXIa inhibitor asundexian”. Bayer (Press release). 2022-08-28. Retrieved 2023-12-27.
- “AntiCoagulation via Inhibition of FXIa by the Oral Compound BAY 2433334 – Non-cardioembolic Stroke”. American College of Cardiology. Retrieved 2023-12-26.
- Rao, Sunil V.; Kirsch, Bodo; Bhatt, Deepak L.; Budaj, Andrzej; Coppolecchia, Rosa; Eikelboom, John; James, Stefan K.; Jones, W. Schuyler; Merkely, Bela; Keller, Lars; Hermanides, Renicus S.; Campo, Gianluca; Ferreiro, José Luis; Shibasaki, Taro; Mundl, Hardi (2022-10-18). “A Multicenter, Phase 2, Randomized, Placebo-Controlled, Double-Blind, Parallel-Group, Dose-Finding Trial of the Oral Factor XIa Inhibitor Asundexian to Prevent Adverse Cardiovascular Outcomes After Acute Myocardial Infarction”. Circulation. 146 (16): 1196–1206. doi:10.1161/CIRCULATIONAHA.122.061612. hdl:11392/2520330. ISSN 0009-7322. PMID 36030390.
- “The Next Wave of Anticoagulation: Results of PACIFIC-AF and the Future Role of Factor XIa Inhibition in Atrial Fibrillation”. American College of Cardiology. Retrieved 2023-12-26.
- “OCEANIC-AF study stopped early due to lack of efficacy”. Bayer (Press release). 2023-11-19. Retrieved 2023-12-27.
- Piccini, Jonathan P.; Patel, Manesh R.; Steffel, Jan; Ferdinand, Keith; Van Gelder, Isabelle C.; Russo, Andrea M.; Ma, Chang-Sheng; Goodman, Shaun G.; Oldgren, Jonas; Hammett, Christopher; Lopes, Renato D.; Akao, Masaharu; De Caterina, Raffaele; Kirchhof, Paulus; Gorog, Diana A.; Hemels, Martin; Rienstra, Michiel; Jones, W. Schuyler; Harrington, Josephine; Lip, Gregory Y.H.; Ellis, Stephen J.; Rockhold, Frank W.; Neumann, Christoph; Alexander, John H.; Viethen, Thomas; Hung, James; Coppolecchia, Rosa; Mundl, Hardi; Caso, Valeria (2025). “Asundexian versus Apixaban in Patients with Atrial Fibrillation”. New England Journal of Medicine. 392 (1): 23–32. doi:10.1056/NEJMoa2407105. hdl:2066/315752. PMID 39225267.
- “Ictus ischemico, i risultati della ricerca su un nuovo farmaco sperimentale: recidive ridotte del 26%”. Ospedale Maggiore di Bologna (in Italian).
- “Bayer’s asundexian demonstrated a substantial 26% reduction in stroke after a non-cardioembolic ischemic stroke or high-risk transient ischemic attack, with no increase in ISTH major bleeding versus placebo”. Bayer.
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 | |
| Clinical data | |
|---|---|
| Trade names | Sunharbo |
| Other names | BAY-2433334; BAY2433334 |
| Legal status | |
| Legal status | US: ℞-only |
| Identifiers | |
| IUPAC name | |
| CAS Number | 2064121-65-7 |
| PubChem CID | 135206011 |
| ChemSpider | 115009501 |
| UNII | LA585UM8DE |
| KEGG | D12838 |
| Chemical and physical data | |
| Formula | C26H21ClF4N6O4 |
| Molar mass | 592.94 g·mol−1 |
| 3D model (JSmol) | Interactive image |
| SMILES | |
| InChI | |
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