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Last update 21 Oct 2026
Buloxibutid
Last update 21 Oct 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- |
RegulationFast Track (United States), Orphan 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
13
Clinical Trials associated with BuloxibutidCTIS2026-526135-18-00
A randomised, open-label, single-centre, drug-drug-interaction trial to evaluate the impact of carboxylesterase 2 (CES2)- and CYP3A4-inhibition on the pharmacokinetics of buloxibutid in healthy volunteers
CTIS2025-520702-35-00
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.
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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242
Literatures (Medical) associated with Buloxibutid01 Jan 2027EXPERIMENTAL NEUROLOGY
C21 ameliorates microglial ferroptosis and neuronal apoptosis after ischemic brain injury by activating the METTL3/USP18/FASN axis
Article
Author: Huang, You ; Zeng, Qingfan ; Sheng, Duanyang ; Zhou, Xinqian ; Wu, Yijiu ; Huo, Xufang
BACKGROUND:
Microglial ferroptosis is a key risk factor promoting neuroinflammation after ischemic brain injury (IBI). Although Compound 21 (C21) has neuroprotective and anti-inflammatory properties, its role in modulating microglial ferroptosis in IBI remains unexplored.
METHODS:
IBI was induced in C57BL/6 mice via transient middle cerebral artery occlusion (tMCAO). Parallelly, an in vitro oxygen-glucose deprivation (OGD) model was established using BV2 microglial cells to mimic ischemic conditions. Gene and protein expression levels were quantified using quantitative real-time polymerase chain reaction (qRT-PCR), western blot, and immunofluorescence staining. Cell viability and apoptosis were assessed using cell counting kit-8 (CCK-8) assay and flow cytometry, respectively. The interactions between methyltransferase-like 3 (METTL3), ubiquitin-specific peptidase 18 (USP18), and fatty acid synthase (FASN) were analyzed by RNA immunoprecipitation (RIP) and co-immunoprecipitation (Co-IP) assays. The ubiquitination of FASN was assessed by immunoprecipitation (IP) assay. The N6-methyladenosine (m6A) modification of USP18 mRNA was analyzed by m6A RNA immunoprecipitation (Me-RIP) and dual-luciferase reporter assays.
RESULTS:
C21 treatment alleviated neuroinflammation and neuronal apoptosis in IBI models by inhibiting microglial ferroptosis. Mechanistically, C21 upregulated USP18 via m6A-dependent mRNA stabilization through increasing METTL3 expression. In addition, C21 stabilized FASN protein through promoting USP18-mediated deubiquitination. Functional experiments further demonstrated that C21 ameliorated microglial ferroptosis and neuronal apoptosis after IBI by activating the METTL3/USP18/FASN axis.
CONCLUSION:
C21 ameliorated neuroinflammation and neuronal apoptosis following IBI by inhibiting microglial ferroptosis through activating the METTL3/USP18/FASN axis. Our findings provide mechanistic insights into the protective role of C21 in IBI and establish a preclinical foundation for further evaluation of its therapeutic potential.
01 Nov 2026Acta Physiologica
Targeted Metabolomics Reveals a Metabolic Signature Derived From the Stimulation of Cells With the Specific
AT
2
R
Agonist
C21
Article
Author: Bajicoff, Sofía ; Jaber, Zahraa ; Narváez Pardo, Jorge Andrés ; Gerling, Leonie ; Dominici, Fernando Pablo ; Hannibal, Luciana ; Oppong‐Danquah, Ernest ; Schumann, Anke
ABSTRACT:
Aim:
Despite increasing evidence for the cardiometabolic protective effects of angiotensin II Type 2 receptor (AT
2
R) activation, the underlying molecular mechanisms remain incompletely understood. This study aimed to determine how AT
2
R activation modulates cellular metabolism and to identify pathways relevant to its tissue‐protective actions.
Methods:
3T3‐L1 adipocytes, endothelial cells, and renal proximal tubular epithelial cells were treated with the specific AT
2
R agonist Compound 21 (C21). Targeted liquid chromatography–tandem mass spectrometry was used to quantify amino acids and metabolites involved in energy metabolism and redox homeostasis. Functional analyses included nitrate/nitrite determination and cystathionine β‐synthase (CBS) activity.
Results:
Compound 21 induced shared and cell type‐specific metabolic changes. Arginine, citrulline, glucose, and glyceraldehyde 3‐phosphate increased consistently across all cell types, whereas citrate decreased. Sulfur‐containing metabolites and glutathione‐related intermediates increased predominantly in adipocytes and renal cells. Pathway analysis highlighted three metabolic axes affected by C21: arginine biosynthesis, central carbon metabolism, and amino acid‐linked redox pathways. Functionally, C21 increased nitrate/nitrite accumulation in BAECs and CBS activity in RPTECs.
Conclusion:
Treatment with C21 was associated with a conserved metabolic signature across adipocytes, renal epithelial cells, and endothelial cells involving arginine biosynthesis, central carbon metabolism, and amino acid‐linked redox homeostasis. While the response differed among cell types, coordinated changes in arginine, citrulline, glucose, glyceraldehyde 3‐phosphate, citrate, and GSH‐related metabolites suggest that AT
2
R signaling is associated with cellular pathways involved in nitric oxide metabolism, energy metabolism, and redox homeostasis. Increased NOx production in BAECs and CBS activity in RPTECs support the cell type‐specific metabolic effects of C21.
01 Sep 2026Cell reports methods
Off-target effects of DREADD ligands revealed by an anesthesia emergence paradigm in mice
Article
Author: Humanes-Valera, Desire ; Foffani, Guglielmo ; Moreno-Gomez, Miryam
Designer receptors exclusively activated by designer drugs (DREADDs) enable reversible control of specific neural circuits, but the pharmacological neutrality of their ligands is increasingly questioned. Here, we introduce an anesthesia emergence paradigm to systematically assess the off-target effects of DREADD ligands in DREADD-naive mice. We show that intraperitoneal administration of clozapine N-oxide (CNO), compound 21 (C21), or deschloroclozapine (DCZ) delays motor recovery from isoflurane anesthesia. CNO produced the largest delay, likely due to its back-conversion to clozapine. DCZ showed the smallest effect magnitude, although its difference from C21 remained inconclusive. We then show that subcutaneous administration, which should reduce clozapine back-conversion, reduces the CNO-induced recovery delay to levels comparable to those of C21. Finally, we provide a freely available, deep-learning-based automated behavioral pipeline that integrates the anesthesia emergence paradigm with a reproducible analysis tool for future studies. Together, these results underscore the importance of accounting for ligand off-target effects through careful dose selection and DREADD-free, ligand-treated controls in chemogenetic experiments.
86
News (Medical) associated with Buloxibutid13 Oct 2026
Phase 2Orphan DrugFast Track
30 Sep 2026
Orphan DrugFast TrackPhase 2
17 Sep 2026
Orphan DrugPhase 2Fast Track
100 Deals associated with Buloxibutid
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External Link
| KEGG | Wiki | ATC | Drug Bank |
|---|---|---|---|
| D13133 | - | - | - |
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) | uwixqhwnbz = ujwqbkfcmo sqwbdvorln (ltriscopbw, csfiayrjbf - kkleqgdtjc) View more | - | 23 May 2025 | ||
(C21 100 mg BID) | onntzrwoca(hrlldlirtn) = mzhyxxsolo vbpaxjzewg (lsvlsfwvtm, defeygajcb - rjootwklrv) View more | ||||||
Phase 1 | - | 5 | (C21 3 ug/Min) | pbwypegeuh(lyyzstltmv) = vxwitlolou ltkmpbccap (cdslsznisg, 24.3) View more | - | 23 Apr 2025 | |
(C21 10 ug/Min) | pbwypegeuh(lyyzstltmv) = tnzksjsegw ltkmpbccap (cdslsznisg, 5.5) View more | ||||||
Phase 1 | 11 | (C21 Treatment) | sbjhddueue(gtmcanflpt) = ammvsauofy rtlfkwhjyq (roteikjfhx, 0.062) View more | - | 12 Nov 2024 | ||
placebo (Placebo Treatment) | sbjhddueue(gtmcanflpt) = axpsykgzos rtlfkwhjyq (roteikjfhx, 0.062) View more | ||||||
Phase 2 | 46 | dzzxwtizqy(nalafszjuz) = pxvtcrsmyz vluxmfynoq (jpmcuzuvez, -150 to +50) View more | Positive | 29 Apr 2024 | |||
Phase 3 | 272 | (C21 Treatment) | ypzvrhoiwd = iqcizvhiek rconzupgbe (wtzintlaqv, bsovoblasz - gcfnpvtknj) View more | - | 14 Dec 2023 | ||
placebo (Placebo Treatment) | ypzvrhoiwd = cfcfzjbtwd rconzupgbe (wtzintlaqv, drwxendcsn - bpzcbcachz) View more | ||||||
Not Applicable | - | C21 100 mg twice daily | jxkdiodmzj(blksdkcvgv) = 3 SAE's none of which were treatment related inclusive of 1 death (COVID-19) nzzrpnlpjh (yfnrtpykrp ) View more | - | 21 May 2023 | ||
Phase 2 | 20 | placebo (Placebo) | ppgcznpyyg(uzzgsermsm) = phfhuazdzz dzrvfuxxms (szztvwetlx, 4.36) View more | - | 18 May 2023 | ||
(C21 200 mg) | ppgcznpyyg(uzzgsermsm) = aqsgieuhvx dzrvfuxxms (szztvwetlx, 7.68) View more | ||||||
Phase 2 | 45 | rorfhshadv(xxbuztssgb) = rvjveplvll vrxgnyadlf (ohmupuvjvk ) View more | Positive | 05 Nov 2022 | |||
Phase 2 | 21 | fcgubyxuxa(ukqfkjapoo) = no signals of gastro-intestinal toxicity picuyetsjy (iifqdkvdne ) View more | Positive | 04 Sep 2022 | |||
Phase 2 | COVID-19 NT-proBNP | 206 | ylnjkqhxqp(wapppdhjvj) = nihcitoduz uflgvetbpi (hxphmxdqdh ) | - | 29 Aug 2022 | ||
Placebo | ylnjkqhxqp(wapppdhjvj) = bsvlpbmtoz uflgvetbpi (hxphmxdqdh ) |
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