A Phase IIa Open Label Study Evaluating the Preliminary Efficacy of Intratumoural Tigilanol Tiglate in Advanced And/or Metastatic Soft Tissue Sarcoma of the Extremities and Body Wall.

A Phase IIa open label study evaluating the preliminary efficacy of intratumoural tigilanol tiglate in advanced and/or metastatic soft tissue sarcoma of the extremities and body wall.

开始日期2023-04-13

申办/合作机构

Qbiotics Pty Ltd.

NCT05608876

/ Recruiting临床2期

A Phase II, Open Label, Single Arm Study To Assess The Efficacy Of Intratumoral Tigilanol Tiglate In Various Head And Neck Solid Malignancies

A Phase II, open label, single arm study to assess the efficacy of intratumoural tigilanol tiglate in various head and neck solid malignancies.

开始日期2022-11-03

申办/合作机构

Qbiotics Pty Ltd.

NCT05234437

/ Terminated临床2期

A Phase IIb, Multicentre, Open Label Study to Evaluate the Effectiveness, Safety and Tolerability of Intratumoural Tigilanol Tiglate in Adult Participants With Stage IIIB to IV M1c Melanoma

A phase IIb, multicentre, open label study to evaluate the effectiveness, safety, and tolerability of intratumoural tigilanol tiglate in adult participants with Stage IIIB to IV M1c melanoma

开始日期2022-03-09

申办/合作机构

Qbiotics Pty Ltd.

100 项与 Tigilanol tiglate 相关的临床结果

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100 项与 Tigilanol tiglate 相关的转化医学

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100 项与 Tigilanol tiglate 相关的专利（医药）

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项与 Tigilanol tiglate 相关的文献（医药）

2025-01-24·Science Advances

Synthesis and preclinical evaluation of tigilanol tiglate analogs as latency-reversing agents for the eradication of HIV

Article

作者: Hamad, Jennifer L. ; Wender, Paul A. ; Moran, Jose A. ; Zack, Jerome A. ; McAteer, Owen D. ; Marsden, Matthew D. ; Gentry, Zachary O. ; Kim, Jocelyn T.

Tigilanol tiglate (EBC-46) is a selective modulator of protein kinase C (PKC) isoforms that is Food and Drug Administration (FDA) approved for the treatment of mast cell tumors in canines with up to an 88% cure rate. Recently, it has been FDA approved for the treatment of soft tissue sarcomas in humans. The role of EBC-46 and, especially, its analogs in efforts to eradicate HIV, treat neurological and cardiovascular disorders, or enhance antigen density in antigen-targeted chimeric antigen receptor–T cell and chimeric antigen receptor–natural killer cell immunotherapies has not been reported. Enabled by our previously reported scalable synthesis of EBC-46, we report herein the systematic design, synthesis, and evaluation of EBC-46 analogs, including those inaccessible from the natural source and their PKC affinities, ability to translocate PKC, nuclear factor κB activity, and efficacy in reversing HIV latency in Jurkat-Latency cells. Leading analogs show exceptional PKC affinities, isoform selectivities, and functional activities, serving as promising candidates for therapeutic applications.

2024-12-31·OncoImmunology

Immunogenic oncolysis by tigilanol tiglate

Article

作者: Kroemer, Guido ; Lizarralde-Guerrero, Manuela ; Pol, Jonathan G.

Tigilanol tiglate is an oncolytic small molecule that is undergoing clinical trials. A recent study revealed the capacity of this pyroptosis inducer to elicit hallmarks of immunogenic cell death. In addition, intratumoral injection of tigilanol tiglate can sensitize subcutaneous cancers to subsequent immune checkpoint inhibitors targeting CTLA-4 alone or in combination with PD-1.

2024-12-01·BIOCHEMICAL PHARMACOLOGY

Epoxytiglianes induce keratinocyte wound healing responses via classical protein kinase C activation to promote skin re-epithelialization

Article

作者: Johns, Jenny P. ; Dally, Jordanna ; Steadman, Robert ; Moses, Rachael L. ; Gordon, Victoria ; Boyle, Glen M. ; Johns, Jenny P ; Boyle, Glen M ; Knäuper, Vera ; Reddell, Paul ; Moseley, Ryan ; Woods, Emma L ; Moses, Rachael L ; Woods, Emma L.

Epoxytiglianes are a novel class of diterpene esters. The prototype epoxytigliane, EBC-46 (tigilanol tiglate), is a potent anti-cancer agent in clinical development for local treatment of a range of human and animal tumors. EBC-46 also consistently promotes wound re-epithelialization at the treatment sites, mediated via activation of classical protein kinase C (PKC) isoforms. We have previously shown that epoxytiglianes stimulate proliferative and wound repopulation responses in immortalized human skin keratinocytes (HaCaTs) in vitro, abrogated by pan-PKC inhibitor, bisindolylmaleimide-1. In this study, we further investigate the specific PKC isoforms responsible for inducing such wound healing responses, following HaCaT treatment with 1.51 nM-15.1 µM EBC-46 or analogue, EBC-211. Classical PKC inhibition by GӦ6976 (1 μM), significantly attenuated epoxytigliane induced, HaCaT proliferation and wound repopulation at all epoxytigliane concentrations. PKC-βI/-βII isoform inhibition by enzastaurin (1 μM), significantly inhibited HaCaT proliferation and wound repopulation responses induced by both epoxytiglianes, especially at 1.51-151 nM. PKC-α inhibitor, Ro 31-8220 mesylate (10 nM), exerted lesser inhibitory effects on HaCaT responses. Epoxytigliane changes in key keratin (KRT17) and cell cycle (cyclin B1, CDKN1A) protein levels were partly attenuated by GӦ6976 and enzastaurin. GӦ6976 also inhibited increases in matrix metalloproteinase (MMP-1, MMP-7, MMP-10) activities. Phospho-PKC (p-PKC) studies confirmed that epoxytiglianes transiently activated classical PKC isoforms (p-PKCα, p-PKC-βI/-βII, p-PKCγ) in a dose- and time-dependent manner. By identifying how epoxytiglianes stimulate classical PKCs to facilitate keratinocyte healing responses and re-epithelialization, these findings support further epoxytigliane development as topical therapeutics for clinical situations involving impaired re-epithelialization, such as non-healing wounds in skin.

项与 Tigilanol tiglate 相关的新闻（医药）

2024-02-16

·Pharmaceutical Technology

QBiotics wins FDA orphan status for rainforest-derived cancer drug

Tigilanol tiglate is a chemical found in the seeds of the pink fruit of the blushwood tree. Image credit: Shutterstock/petrmalinak. Australian biotech QBiotics has won an orphan drug designation for a drug based on a chemical obtained from the blushwood tree, which is being investigated as a treatment for a rare group of cancers called soft tissue sarcoma . Qbiotics will now be in line for tax credits for US-based clinical trials and, if the therapy is approved, the potential for seven years of market exclusivity for the given indication. A veterinary formulation of the drug, tigilanol tiglate, is already approved for use in the US, UK, and Australia under the trade name Stelfonta. QBiotics started life as EcoBiotics, which was established in 2000 to discover potential drugs from Queensland’s tropical rainforest. QBiotics itself was founded in 2004 as a subsidiary of EcoBiotics, and the two groups merged in 2017. The company has signed several biodiscovery agreements covering the rainforest areas in the country in the past decade. The company has not disclosed how it scales tigilanol tiglate – a chemical found in the seeds of the pink fruit of the blushwood tree. Tigilanol tiglate is administered directly into a solid tumour mass by intratumoural injection. See Also: Regeneron and Sanofi’s Dupixent bags fifth drug label in Japan Dragonfly and Gilead enter partnership for cancer therapy The drug candidate works by disrupting blood vessels keeping the tumour alive and directly killing cancer cells by oncosis. QBiotics states that tigilanol tiglate also induces tumour site healing and can even be administered systemically to induce indirect anti-tumour responses. QBitotics’ Phase II clinical trial in soft tissue sarcoma (NCT05755113) is ongoing with ten participants estimated to be enrolled. The primary endpoint is tumour ablation. Soft tissue sarcoma is the broad term for rare cancers that grow in soft tissues anywhere in the body. There are several targeted therapies approved to treat soft tissue sarcoma – last month, Adaptimmune applied to the FDA for approval of afami-cel. If approved, it would be the first T-cell therapy for a type of soft tissue sarcoma. QBiotics is exploring its lead candidate as a monotherapy and in combination with MSD’s checkpoint inhibitor Keytruda (pembrolizumab) following a partnership with the company signed in 2020. A Phase I/II trial with the treatment paradigm is ongoing in advanced melanoma. As per the company, a dose-escalation Phase I trial in 22 patients with a range of solid tumours treated with tigilanol tiglate, demonstrated a complete response of 18%. Stable disease was seen in 64% of the treatment group, and the remaining 22% demonstrated partial response. QBiotics is conducting further clinical trials with tigilanol tiglate as a monotherapy in squamous cell carcinoma, head and neck tumours (NCT05608876), and advanced melanoma (NCT05234437). A model by GlobalData estimates that there were just over 125,000 new cases of soft tissue sarcoma globally in 2023, with incidence growing at 0.54% per year. GlobalData is the parent company of Pharmaceutical Technology.

临床1期临床结果孤儿药细胞疗法临床2期

2023-05-31

·PRNewswire

QBIOTICS TO PRESENT AT SACHS 9TH ANNUAL IMMUNO-ONCOLOGY INNOVATION FORUM AND THE BIO INTERNATIONAL CONVENTION

BRISBANE, Australia, May 31, 2023 /PRNewswire/ -- QBiotics Group Limited ( QBiotics), a clinical stage life sciences company developing novel small molecule anticancer and wound healing pharmaceuticals is pleased to announce that Richard Godfrey will present to potential partners and investors at the Sachs 9th Annual Immuno-Oncology Innovation Forum and the BIO International Convention, both being held in the US through June 2023. Mr Godfrey, representing QBiotics in Business Development, Licensing and Partnerships, will provide an update on the Company's human and veterinary programmes in oncology and wound healing. The presentations will include recent phase I safety and efficacy data with Tigilanol tiglate (TT) in cancer patients and details of two ongoing phase II studies in later stage patients with Head and Neck cancer and Soft Tissue Sarcoma, being treated with TT. The Sachs 9th Annual Immuno-Oncology Innovation Forum for Business Development, Licensing and investment is at the Waldorf Astoria Chicago Hotel, USA Presentation time: 2 June 2023, at 11:40 AM Central Daylight Time (GMT-5)). Venue: The Faulkner Room Recorded sessions will also be added to the event portal as available on demand during the virtual week, which takes place from 13 – 15 June EDT. The BIO International Convention takes place at the Boston Convention & Exhibition Center, USA on 5 – 8 June 2023. Presentation time: 5 June at 12:30 PM Eastern Daylight Time (EDT). Venue: Session Room 103 Dr Victoria Gordon, CEO of QBiotics commented, "It is an important part of QBiotics' partner and investor engagement strategy to attend ASCO and present at the high-profile satellite SACHS immune oncology forum, as well as presenting our company at the BIO International Convention. We look forward to discussing our lead assets, tigilanol tiglate in the human and veterinary oncology space, and also sharing more information on our second pipeline candidate EBC-1013, which has shown compelling early promise in wound healing." Any potential partners or investors interested in engaging around QBiotics and its programmes are invited to reach out directly or via the one-on-one conference partnering systems. ABOUT QBIOTICS QBiotics is an unlisted public Australian life sciences company that discovers and develops pharmaceuticals derived from nature to address unmet medical needs in humans and companion animals. Our current clinical focus is on novel treatments for cancer and debilitating chronic wounds. QBiotics' business model is to develop products that have applications in both veterinary and human markets. Success in the veterinary programme validates QBiotics technology and de-risks human development while having the potential to generate early revenue. QBiotics' lead oncology product, tigilanol tiglate, is a small molecule targeting a range of solid tumours and is currently in human clinical Phase II development in Head and Neck cancer and Soft Tissue Sarcoma, at sites in USA, UK and Australia. A veterinary formulation of tigilanol tiglate is registered and marketed as an oncology pharmaceutical, under the trade name STELFONTA®, in the USA, Europe, the UK and Australia. QBiotics' lead wound healing product EBC-1013, is a small molecule targeting a range of wounds including chronic and acute wounds and burns. Preparation is in progress for a first-in-human Phase I/IIa clinical trial in patients with stubborn venous leg ulcers. FURTHER INFORMATION Dr Victoria Gordon CEO & Managing Director, QBIOTICS GROUP [email protected] Richard Godfrey Business Development, Licensing and Partnering [email protected] MEDIA JANE LOWE, IR DEPARTMENT ENQUIRIES [email protected] or +61 411 117 774 SOURCE QBiotics Group Limited

临床2期临床1期

2023-05-31

·BioSpace

Qbiotics to Present at Sachs 9th Annual Immuno-Oncology Innovation Forum and the Bio International Convention

BRISBANE, Australia, May 31, 2023 /PRNewswire/ -- QBiotics Group Limited (QBiotics), a clinical stage life sciences company developing novel small molecule anticancer and wound healing pharmaceuticals is pleased to announce that Richard Godfrey will present to potential partners and investors at the Sachs 9th Annual Immuno-Oncology Innovation Forum and the BIO International Convention, both being held in the US through June 2023. Mr Godfrey, representing QBiotics in Business Development, Licensing and Partnerships, will provide an update on the Company's human and veterinary programmes in oncology and wound healing. The presentations will include recent phase I safety and efficacy data with Tigilanol tiglate (TT) in cancer patients and details of two ongoing phase II studies in later stage patients with Head and Neck cancer and Soft Tissue Sarcoma, being treated with TT. The Sachs 9th Annual Immuno-Oncology Innovation Forum for Business Development, Licensing and investment is at the Waldorf Astoria Chicago Hotel, USA Presentation time: 2 June 2023, at 11:40 AM Central Daylight Time (GMT-5)). Venue: The Faulkner Room Recorded sessions will also be added to the event portal as available on demand during the virtual week, which takes place from 13 – 15 June EDT. The BIO International Convention takes place at the Boston Convention & Exhibition Center, USA on 5 – 8 June 2023. Presentation time: 5 June at 12:30 PM Eastern Daylight Time (EDT). Venue: Session Room 103 Dr Victoria Gordon, CEO of QBiotics commented, "It is an important part of QBiotics' partner and investor engagement strategy to attend ASCO and present at the high-pro SACHS immune oncology forum, as well as presenting our company at the BIO International Convention. We look forward to discussing our lead assets, tigilanol tiglate in the human and veterinary oncology space, and also sharing more information on our second pipeline candidate EBC-1013, which has shown compelling early promise in wound healing." Any potential partners or investors interested in engaging around QBiotics and its programmes are invited to reach out directly or via the one-on-one conference partnering systems. ABOUT QBIOTICS QBiotics is an unlisted public Australian life sciences company that discovers and develops pharmaceuticals derived from nature to address unmet medical needs in humans and companion animals. Our current clinical focus is on novel treatments for cancer and debilitating chronic wounds. QBiotics' business model is to develop products that have applications in both veterinary and human markets. Success in the veterinary programme validates QBiotics technology and de-risks human development while having the potential to generate early revenue. QBiotics' lead oncology product, tigilanol tiglate, is a small molecule targeting a range of solid tumours and is currently in human clinical Phase II development in Head and Neck cancer and Soft Tissue Sarcoma, at sites in USA, UK and Australia. A veterinary formulation of tigilanol tiglate is registered and marketed as an oncology pharmaceutical, under the trade name STELFONTA®, in the USA, Europe, the UK and Australia. QBiotics' lead wound healing product EBC-1013, is a small molecule targeting a range of wounds including chronic and acute wounds and burns. Preparation is in progress for a first-in-human Phase I/IIa clinical trial in patients with stubborn venous leg ulcers. FURTHER INFORMATION Dr Victoria Gordon CEO & Managing Director, QBIOTICS GROUP communications@qbiotics.com Richard Godfrey Business Development, Licensing and Partnering Richard.Godfrey@qbiotics.com MEDIA JANE LOWE, IR DEPARTMENT ENQUIRIES jane.lowe@irdepartment.com.au or +61 411 117 774 View original content: SOURCE QBiotics Group Limited

临床2期临床1期

100 项与 Tigilanol tiglate 相关的药物交易

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外链

KEGG	Wiki	ATC	Drug Bank
D11191	Tigilanol tiglate	-	-

研发状态

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适应症	最高研发状态	国家/地区	公司	日期
转移性软组织肉瘤	临床2期	美国	Qbiotics Pty Ltd.	2023-04-13
鼻肿瘤	临床2期	澳大利亚	Qbiotics Pty Ltd.	2022-11-03
鼻肿瘤	临床2期	英国	Qbiotics Pty Ltd.	2022-11-03
唾液腺肿瘤	临床2期	澳大利亚	Qbiotics Pty Ltd.	2022-11-03
唾液腺肿瘤	临床2期	英国	Qbiotics Pty Ltd.	2022-11-03
头颈部鳞状细胞癌	临床2期	澳大利亚	Qbiotics Pty Ltd.	2022-11-03
头颈部鳞状细胞癌	临床2期	英国	Qbiotics Pty Ltd.	2022-11-03
黑色素瘤	临床2期	澳大利亚	Qbiotics Pty Ltd.	2022-03-09
不可切除的黑色素瘤	临床2期	澳大利亚	Qbiotics Pty Ltd.	2021-05-07

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临床结果

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研究	分期	人群特征	评价人数	分组	结果	评价	发布日期


NCT05755113 (ESMO2024) 人工标引	临床2期	软组织肉瘤末线	5	Intratumoural Tigilanol Tiglate (TT)	鬱襯構憲鬱襯鏇醖築憲(廠鑰構糧繭鑰淵遞築繭) = 積廠鹹鏇顧夢網選網廠構餘鏇築膚遞築簾簾鏇 (廠齋範淵鬱膚醖鏇鑰構 ) 更多	积极	2024-09-14