Delving into the Latest Updates on Kubutin A with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Kudinoside A, 苦丁茶皂苷A

Target

Taste 2 receptors

Mechanism

Taste 2 receptors agonists

Therapeutic Areas

Immune System DiseasesRespiratory Diseases

Active Indication

AsthmaBronchiectasisPulmonary Disease, Chronic Obstructive

Inactive Indication-

Originator Organization

Shanghai Kaiyi Pharmaceutical Technology Co., Ltd.

Active Organization

Zhejiang Wolwo Bio-Pharmaceutical Co., Ltd.

Shanghai Kaiyi Pharmaceutical Technology Co., Ltd.

Inactive Organization-

Drug Highest PhasePhase 2

First Approval Date-

Regulation-

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Primary objective: To evaluate the efficacy of kubutan saponin A inhalation solution in patients with moderate chronic obstructive pulmonary disease (COPD) for 29 consecutive days. Secondary objective: To evaluate the safety of kubutan saponin A inhalation solution in patients with moderate chronic obstructive pulmonary disease (COPD) for 29 consecutive days.

Start Date16 Apr 2024

Sponsor / Collaborator

Shanghai Kaiyi Pharmaceutical Technology Co., Ltd.

CTR20223064 / CompletedPhase 1

吸入用苦丁皂苷A溶液（KA溶液）单/多次给药在中重度慢性阻塞性肺疾病患者中的开放、安全性和药效学研究

[Translation] An open-label, safety and pharmacodynamic study of single/multiple administrations of inhaled kubutan saponin A solution (KA solution) in patients with moderate to severe chronic obstructive pulmonary disease

主要目的：评价中重度慢性阻塞性肺疾病（COPD）患者单/多次给予吸入用苦丁皂苷A溶液的安全性。次要目的：评价单/多次给予吸入用苦丁皂苷A溶液在中重度COPD患者中的药效学（PD）指标。

[Translation]

Primary objective: To evaluate the safety of single/multiple administrations of inhaled kudingsaponin A solution in patients with moderate to severe chronic obstructive pulmonary disease (COPD). Secondary objective: To evaluate the pharmacodynamic (PD) indexes of single/multiple administrations of inhaled kudingsaponin A solution in patients with moderate to severe COPD.

Start Date14 Dec 2022

Sponsor / Collaborator

Shanghai Kaiyi Pharmaceutical Technology Co., Ltd.

CTR20221380 / CompletedPhase 1

吸入用苦丁皂苷A溶液多次给药在健康志愿者中的随机、双盲、剂量递增、安慰剂平行对照的安全性、耐受性、药代动力学研究

[Translation] A randomized, double-blind, dose-escalation, placebo-controlled safety, tolerability, and pharmacokinetics study of multiple doses of inhaled kudingsaponin A solution in healthy volunteers

主要目的：观察在健康志愿者中多次给予不同剂量吸入用苦丁皂苷A溶液的安全性和耐受性。次要目的：考察多次给予不同剂量吸入用苦丁皂苷A溶液在健康志愿者中的药代动力学特征。

[Translation]

Primary objective: To observe the safety and tolerability of multiple administrations of different doses of inhaled kudingsaponin A solution in healthy volunteers. Secondary objective: To investigate the pharmacokinetic characteristics of multiple administrations of different doses of inhaled kudingsaponin A solution in healthy volunteers.

Start Date23 Jun 2022

Sponsor / Collaborator

Shanghai Kaiyi Pharmaceutical Technology Co., Ltd.

100 Clinical Results associated with Kubutin A

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100 Translational Medicine associated with Kubutin A

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100 Patents (Medical) associated with Kubutin A

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36

Literatures (Medical) associated with Kubutin A

01 Jul 2024·Fitoterapia

Unveiling the anti-vitiligo, anti-inflammatory, and antitumor activities of sesquiterpene coumarins isolated from Ferula kuhistanica

Article

Author: Numonov, Sodik ; Guoruoluo, Yindendzhi ; Ashurov, Khushang ; Turak, Ablajan ; Aisa, Haji Akber

Six undescribed bicyclic sesquiterpene coumarins, kuhistanin A, ferukrin isovalerate, 9'β,12'α - ferukrin isovalerate, (17'E)- 9'α, 12'β - isomarcandin, (17'Z)- 9'α, 12'β - isomarcandin and (17'E) - isomarcandin, together with nine known ones were isolated from the roots of Ferula kuhistanica Korovin. The structures of them were elucidated using NMR and HRESIMS data analysis. The relative configurations of the isolates were confirmed by NOE correlations and NMR calculation. The absolute configurations of them were confirmed by X-ray diffraction analysis and ECD calculation. Anti-vitiligo, anti-inflammatory and cytotoxicity of the isolates were tested. Acetyl feselol, feselol, ferusingensine I and farnesiferol A significantly increased the melanin content at the concentration of 10 μM. (17'E) - 9'α, 12'β - isomarcandin exhibited strong cytotoxicity against HT-29 cell line with IC₅₀ values of 8.94 ± 0.47 μM, and (17'E) - isomarcandin demonstrated strong cytotoxicity against Hela, A549 and HT-29 cell lines with IC₅₀ values of 5.29 ± 0.25, 4.01 ± 0.20, and 4.16 ± 0.21 μM, respectively. This study concluded that, isolated compounds from F. kuhistanica demonstrated strong bioactivity towards anti-vitiligo and cytotoxicity and active compounds are suggested as anti-vitiligo and cytotoxicity agent for future drug development.

01 Mar 2023·Acta Crystallographica Section E Crystallographic Communications

Crystal structures of two 1,2,3,4-tetrahydronaphthalenes obtained during efforts towards the total synthesis of elisabethin A

Article

Author: Enev, Valentin ; Weil, Matthias ; Kaiser, Maximilian ; Gärtner, Peter

The two substituted 1,2,3,4-tetrahydronaphthalenes, methyl (R)-3-{(1R,4S)-6-methoxy-4,7-dimethyl-5,8-bis[(triisopropylsilyl)oxy]-1,2,3,4-tetrahydronaphthalen-1-yl}butanoate, C36H66O5Si2, (2), and methyl (E)-3-{(1R,4S)-8-hydroxy-6-methoxy-4,7-dimethyl-5-[(triisopropylsilyl)oxy]-1,2,3,4-tetrahydronaphthalen-1-yl}acrylate, C26H42O5Si, (8), crystallize in the Sohncke space groups P212121 and P21, respectively, with the absolute structure determined on the basis of anomalous dispersion effects. The configurations of the stereo centres in the 1,2,3,4-tetrahydronaphthalene moiety of (2) and (8) are the same, and the conformation of the non-aromatic part of the ring system is nearly identical. In the crystal of (2), weak non-classical C—H...O interactions consolidate the packing, whereas in (8), intermolecular O—H...O hydrogen-bonding interactions of medium-to-weak strength direct the molecules into Z-shaped strands extending parallel to [010].

28 Jun 2022·Proceedings of the National Academy of SciencesQ1 · CROSS-FIELD

Tas2R activation relaxes airway smooth muscle by release of Gα _t targeting on AChR signaling

Q1 · CROSS-FIELD

Article

Author: Sun, Jie ; Jiang, Zhi-Hui ; Ma, Ming ; Tao, Tao ; Wang, Han ; Wang, Ye ; Yang, Li-Yuan ; Chen, Cai-Ping ; Zhang, Zhong-Liang ; Li, Ye-Qiong ; Zhang, Jian ; Wang, Pei ; Zhu, Min-Sheng ; Chen, Xin ; Zhang, Xue-Na ; Chen, Hua-Qun ; Pan, Yang ; Zhou, Yu-Wei ; Qiu, Tian-Tian

Both chronic obstructive pulmonary disease (COPD) and asthma are severe respiratory diseases. Bitter receptor–mediated bronchodilation is a potential therapy for asthma, but the mechanism underlying the agonistic relaxation of airway smooth muscle (ASM) is not well defined. By exploring the ASM relaxation mechanism of bitter substances, we observed that pretreatment with the bitter substances nearly abolished the methacholine (MCh)-induced increase in the ASM cell (ASMC) calcium concentration, thereby suppressing the calcium-induced contraction release. The ASM relaxation was significantly inhibited by simultaneous deletion of three Gα t proteins, suggesting an interaction between Tas2R and AChR signaling cascades in the relaxation process. Biochemically, the Gα t released by Tas2R activation complexes with AChR and blocks the Gα q cycling of AChR signal transduction. More importantly, a bitter substance, kudinoside A, not only attenuates airway constriction but also significantly inhibits pulmonary inflammation and tissue remodeling in COPD rats, indicating its modulation of additional Gα q -associated pathological processes. Thus, our results suggest that Tas2R activation may be an ideal strategy for halting multiple pathological processes of COPD.

100 Deals associated with Kubutin A

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R&D Status

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Asthma	Phase 2	CN	Shanghai Kaiyi Pharmaceutical Technology Co., Ltd.	16 Apr 2024
Bronchiectasis	Phase 1	CN	Zhejiang Wolwo Bio-Pharmaceutical Co., Ltd.	30 Jan 2022
Pulmonary Disease, Chronic Obstructive	Phase 1	CN	Shanghai Kaiyi Pharmaceutical Technology Co., Ltd.	08 Jul 2021

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


CTR20211313 (NEWS) Manual	Phase 1	Pulmonary Disease, Chronic Obstructive \| Asthma	-	Kubutin A	(safhposjwe) = dzfbihiovo raohudrofy (rsocbeojws ) View more	Positive	19 Aug 2022