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Last update 25 Feb 2026
Buloxibutid
Last update 25 Feb 2026
Overview
Basic Info
Drug Type Small molecule drug |
Synonyms 3-[4-(lH-imidazol-l-ylmethyl)phenyl]-5-(2-methylpropyl) thiophene-2-[(N-butyloxylcarbamate)-sulphonamide] sodium salt, C-21, C21 + [5] |
Target |
Action agonists |
Mechanism AT2R agonists(Angiotensin II receptor type 2 agonists) |
Therapeutic Areas |
Active Indication |
Inactive Indication |
Originator Organization |
Active Organization |
Inactive Organization- |
License Organization |
Drug Highest PhasePhase 3 |
First Approval Date- |
RegulationOrphan Drug (United States), Orphan Drug (European Union), Orphan Drug (Japan) |
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Structure/Sequence
Molecular FormulaC23H29N3O4S2 |
InChIKeyXTEOJPUYZWEXFI-UHFFFAOYSA-N |
CAS Registry477775-14-7 |
Sequence Code 15939045
Related
12
Clinical Trials associated with BuloxibutidCTIS2025-520702-35-00
A randomised, open-label, 5-period, cross-over trial to assess the pharmacokinetics and safety of 3 oral solid formulations of buloxibutid (C21) in healthy male and female participants
NCT06588686
A Randomized, Double-blind, Placebo-controlled, Parallel-group, Multicenter Trial Evaluating the Efficacy and Safety of 2 Doses of Buloxibutid Over 52 Weeks in People With Idiopathic Pulmonary Fibrosis.
NCT05831644
A Randomized, Double-blind, Placebo-controlled, 2-way Cross-over Trial Evaluating the Effect of C21 on Endothelial Dysfunction and Safety in Subjects With Type 2 Diabetes Mellitus
100 Clinical Results associated with Buloxibutid
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100 Translational Medicine associated with Buloxibutid
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100 Patents (Medical) associated with Buloxibutid
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222
Literatures (Medical) associated with Buloxibutid01 Feb 2026JOURNAL OF MOLECULAR HISTOLOGY
Protective effects of buloxibutid and empagliflozin on hypertension-induced cardiac and vascular injury in rats
Article
Author: Parlakpinar, Hakan ; Dogru, Feyzi ; Kucukakcali, Zeynep ; Karaca, Elif ; Acet, Ahmet ; Colak, Mehmet ; Ozhan, Onural
This study aims to see the individual and combined effects of Angiotensin II type 2 (AT2) receptor agonist buloxibutid (also known as Compound 21 or C21) and sodium-glucose co-transporter-2 (SGLT-2) inhibitor empagliflozin (EMPA) on effects of hypertension (HT), which is common today, on the heart, and vascular tissue. Male rats of the Sprague Dawley were divided into 5 groups: Control (C) group, HT group, HT + C21 group, HT + EMPA group and HT + C21 + EMPA group. After the protocol was completed, hemodynamic measurements were taken and heart and aorta tissues were evaluated biochemically, histopatologically and immunohistochemically. When the mean blood pressure (BP) values were compared, the mean BP of the HT group increased significantly compared to the C group (p < 0.05). Superoxide dismutase, glutathione and glutathione peroxidase activities in the heart, glutathione and catalase activities in the descending aorta were significantly higher in all treated groups compared to the HT group (p < 0.05). In the HT + C21 + EMPA group, histopathological damage score in hematoxylin-eosin (HE) stained heart sections compared to the HT group showed a decrease in tissue damage but cell infiltration was still observed. When HE staining method was applied, it was determined that the thoracic aorta sections in group C had normal histologic structure. In the HT group, dilatation in some parts and irregularities in elastic lamellae were observed. It was observed that the treated groups were similar to group C. When considering the individual and combined effects of C21 and EMPA, positive results on heart and vascular tissue were observed by hemodynamic, biochemical and histopathological analyses.
01 Feb 2026EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Design, synthesis, and biological evaluation of 2-(benzylthio)-5-(indol-3-yl)-1,3,4-oxadiazole derivatives as tubulin polymerization inhibitors with potential anti-cancer effects
Article
Author: You, Jie ; Xie, Qing ; Shi, Jing-Yi ; Man, Ruo-Jun ; Dai, Hong ; Yang, Bing ; Zhu, Hai-Liang
Thirty new 2-(benzylthio)-5-(indol-3-yl)-1,3,4-oxadiazole derivatives were designed, synthesized, and evaluated as tubulin inhibitors against cancers. Some target compounds showed relatively strong anti-proliferative activity against HepG2, HeLa, MCF-7, and A549 cells. Among them, the top hit, compound C21, yielded an IC50 value of 0.08 μM against HeLa cells, exhibiting lower cytotoxicity compared to 293T cells. Tubulin polymerization inhibition assay indicated that the inhibitory activity of compound C21 (IC50: 1.59 ± 0.66 μM) was stronger than that of Colchicine (IC50: 2.52 ± 0.23 μM). Mechanism studies demonstrated that compound C21 could arrest cell cycle at the G2/M phase and induce tumor cell apoptosis in a dose- and time-dependent manner. The confocal imaging further demonstrated that compound C21 could inhibit tubulin polymerization, similar to Colchicine. Moreover, compound C21 showed excellent in vivo anti-tumor potency in a human cervical cancer xenograft mouse model with an inhibitory rate of 80.51 %, which was better than the CA-4P group (49.22 %) and the lower dose group (69.52 %). Furthermore, the docking simulation visualized the possible binding pattern of compound C21 into tubulin. Finally, the information provided in this study will be helpful for the future development of tubulin-related anti-cancer drugs.
02 Jan 2026EXPERT OPINION ON INVESTIGATIONAL DRUGS
Investigational insights into the potential of angiotensin type II receptor agonists as therapeutics for idiopathic pulmonary fibrosis
Review
Author: Young, Olivia N. ; Widdop, Robert E. ; Bourke, Jane E.
INTRODUCTION:
Current standard-of-care for idiopathic pulmonary fibrosis is limited to nintedanib and pirfenidone, which only slow the progressive loss of lung function and have significant adverse effects that are intolerable to many patients. There is therefore a significant unmet need for alternative treatments for this incurable disease.
AREAS COVERED:
This review describes emerging evidence implicating dysregulation of the renin-angiotensin system in IPF pathogenesis, and both pre-clinical and recent clinical data supporting activation of the anti-fibrotic AT2R as a promising therapeutic strategy. The efficacy of AT2R agonists across pre-clinical models of both IPF and relevant lung diseases is discussed, with a particular focus on favorable findings with the AT2R agonist C21 (buloxibutid), leading to its current clinical trials for IPF.
EXPERT OPINION:
Rapid translation of C21 (now named buloxibutid), the first-in-class orally available AT2R agonist, to early phase clinical trials for IPF have established its safety and disease-modifying potential. Ongoing development of novel, more highly selective AT2R agonists may deliver the same clinical benefit as C21 with reduced off-target effects. The AT2R drug class offers great promise as novel therapeutics, potentially extending beyond IPF to other inflammatory and fibrotic lung diseases.
64
News (Medical) associated with Buloxibutid20 Nov 2025
Orphan DrugFast TrackPhase 2
12 Nov 2025
100 Deals associated with Buloxibutid
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R&D Status
10 top R&D records. to view more data
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| Indication | Highest Phase | Country/Location | Organization | Date |
|---|---|---|---|---|
| COVID-19 | Phase 3 | United States | 16 Sep 2021 | |
| COVID-19 | Phase 3 | Argentina | 16 Sep 2021 | |
| COVID-19 | Phase 3 | Brazil | 16 Sep 2021 | |
| COVID-19 | Phase 3 | Colombia | 16 Sep 2021 | |
| COVID-19 | Phase 3 | Czechia | 16 Sep 2021 | |
| COVID-19 | Phase 3 | India | 16 Sep 2021 | |
| COVID-19 | Phase 3 | Philippines | 16 Sep 2021 | |
| COVID-19 | Phase 3 | Russia | 16 Sep 2021 | |
| COVID-19 | Phase 3 | South Africa | 16 Sep 2021 | |
| COVID-19 | Phase 3 | Ukraine | 16 Sep 2021 |
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Clinical Result
Clinical Result
Indication
Phase
Evaluation
View All Results
Phase 2 | 52 | (C21 100 mg BID, SAS) | ezhrfgzfxq = fvkuhnlfnp cdzcqvyves (ereyfqpdxj, fpvkgudxqj - yyxpdxzqzn) View more | - | 23 May 2025 | ||
(C21 100 mg BID) | lucbgghqwf(oateocpmcn) = cdwwvqyfxs hijpxwepws (cvhhnufpjn, mxrhfmsmwl - fkabpypgxi) View more | ||||||
Phase 1 | - | 5 | (C21 3 ug/Min) | zkzhlcsurx(ovgbvgcxjx) = iddjynqggn udvssljzyf (fyfpuzhexu, 24.3) View more | - | 23 Apr 2025 | |
(C21 10 ug/Min) | zkzhlcsurx(ovgbvgcxjx) = cobnzddcwh udvssljzyf (fyfpuzhexu, 5.5) View more | ||||||
Phase 1 | 11 | (C21 Treatment) | xakwpnqopq(bdcqzbdjag) = tbaigznimw lriabybrxj (lwvikviafn, 0.062) View more | - | 12 Nov 2024 | ||
placebo (Placebo Treatment) | xakwpnqopq(bdcqzbdjag) = lqcafkqcdc lriabybrxj (lwvikviafn, 0.062) View more | ||||||
Phase 2 | 46 | mevfeqyutx(towyhswnmc) = eahkwsikdr nunvykwjdm (llwrrrbojn, -150 to +50) View more | Positive | 29 Apr 2024 | |||
Phase 3 | 272 | (C21 Treatment) | ipcstpsjym = tjkwnfyrpa xlinfmqijx (fnlicwercq, usgxbwdzbb - cdmbblesys) View more | - | 14 Dec 2023 | ||
placebo (Placebo Treatment) | ipcstpsjym = gtwubinhzy xlinfmqijx (fnlicwercq, wjajylrmta - ctmplwnmol) View more | ||||||
Not Applicable | - | C21 100 mg twice daily | wdnbbhmipz(chldkamgkz) = 3 SAE's none of which were treatment related inclusive of 1 death (COVID-19) yediehoywt (kxibciofrv ) View more | - | 21 May 2023 | ||
Phase 2 | 20 | placebo (Placebo) | uhgebzlvna(hpazquvpsj) = oflakmmpqd axhqkszcca (jbhjesuvrx, 4.36) View more | - | 18 May 2023 | ||
(C21 200 mg) | uhgebzlvna(hpazquvpsj) = ayddxfogdv axhqkszcca (jbhjesuvrx, 7.68) View more | ||||||
Phase 2 | 45 | msdxfalukm(gvoxpfbpej) = oexgdstuys qsdjqrpufx (rhfvojsqko ) View more | Positive | 05 Nov 2022 | |||
Phase 2 | 21 | obxekkwenv(xuisfcqudj) = no signals of gastro-intestinal toxicity gncuuamzkk (wgqlasrjit ) View more | Positive | 04 Sep 2022 | |||
Phase 2 | COVID-19 NT-proBNP | 206 | bkcgezhewo(dzclsvltbw) = jnxkhotnub mhynvfxvzf (ugqbgelrey ) | - | 29 Aug 2022 | ||
Placebo | bkcgezhewo(dzclsvltbw) = qefoyhpawx mhynvfxvzf (ugqbgelrey ) |
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