This phase I trial tests the safety, side effects, and best dose of dexamethasone when given with azeliragon in managing cerebral edema after surgery (post-resection) in patients with glioblastoma. Cerebral edema is a pathological increase in the water mass contained within the brain interstitial space. Dexamethasone is in a class of medications called corticosteroids. It is used to reduce inflammation and lower the body's immune response to help lessen the side effects of chemotherapy drugs. Azeliragon is an oral RAGE inhibitor. Blocking the RAGE pathway at the time of surgery (peri-operatively) may decrease cerebral edema. Giving dexamethasone with azeliragon may help control post-operative cerebral edema in decreasing doses of concurrently administered dexamethasone.

Start Date15 Aug 2024

Sponsor / Collaborator

City of Hope National Medical Center

[+1]

NCT05789589 / RecruitingPhase 1/2IIT

A Phase I/II Study to Assess Safety and Preliminary Evidence of a Therapeutic Effect of Azeliragon Combined With Stereotactic Radiation Therapy in Patients With Brain Metastases

To determine the safety and efficacy of using the drug azeliragon combined with stereotactic radiosurgery. Specifically, to determine if this combination will lead to improved response in the brain (tumor shrinking in size) and overall tumor control (how long tumor remains controlled).

Start Date17 Nov 2023

Sponsor / Collaborator

Baptist Health South Florida, Inc.

[+2]

NCT05986851 / RecruitingPhase 2

A Phase II Study to Assess Safety and Preliminary Evidence of a Therapeutic Effect of Azeliragon in Patients With MGMT Unmethylated Glioblastoma

This is a phase 2 study to evaluate the safety and preliminary evidence of effectiveness of azeliragon, in combination with radiation therapy, as an initial treatment of a form of glioblastoma. Glioblastoma is a type of brain cancer that grows quickly and can invade and destroy healthy tissue. There's no cure for glioblastoma, which is also known as glioblastoma multiforme. Treatments, including surgery, radiation, and chemotherapy might slow cancer growth and reduce symptoms. New treatments of glioblastoma are needed.

Start Date12 Sep 2023

Sponsor / Collaborator

Cantex Pharmaceuticals, Inc.

[+1]

100 Clinical Results associated with Azeliragon

100 Translational Medicine associated with Azeliragon

100 Patents (Medical) associated with Azeliragon

Literatures (Medical) associated with Azeliragon

13 Jul 2023·NPJ breast cancer

RAGE inhibitor TTP488 (Azeliragon) suppresses metastasis in triple-negative breast cancer.

Article

Author: Mera, Barbara J ; Drews-Elger, Katherine ; McIntosh, Alec ; Kwak, Taekyoung ; Miller, Philip ; Hudson, Barry I ; Magna, Melinda ; Ikeda, Adam ; Takabatake, Masaru ; Lippman, Marc E ; Hwang, Gyong Ha

Triple-negative breast cancer (TNBC) is a highly aggressive and metastatic cancer subtype, which is generally untreatable once it metastasizes. We hypothesized that interfering with the Receptor for Advanced Glycation End-products (RAGE) signaling with the small molecule RAGE inhibitors (TTP488/Azeliragon and FPS-ZM1) would impair TNBC metastasis and impair fundamental mechanisms underlying tumor progression and metastasis. Both TTP488 and FPS-ZM1 impaired spontaneous and experimental metastasis of TNBC models, with TTP488 reducing metastasis to a greater degree than FPS-ZM1. Transcriptomic analysis of primary xenograft tumor and metastatic tissue revealed high concordance in gene and protein changes with both drugs, with TTP488 showing greater potency against metastatic driver pathways. Phenotypic validation of transcriptomic analysis by functional cell assays revealed that RAGE inhibition impaired TNBC cell adhesion to multiple extracellular matrix proteins (including collagens, laminins, and fibronectin), migration, and invasion. Neither RAGE inhibitor impaired cellular viability, proliferation, or cell cycle in vitro. Proteomic analysis of serum from tumor-bearing mice revealed RAGE inhibition affected metastatic driver mechanisms, including multiple cytokines and growth factors. Further mechanistic studies by phospho-proteomic analysis of tumors revealed RAGE inhibition led to decreased signaling through critical BC metastatic driver mechanisms, including Pyk2, STAT3, and Akt. These results show that TTP488 impairs metastasis of TNBC and further clarifies the signaling and cellular mechanisms through which RAGE mediates metastasis. Importantly, as TTP488 displays a favorable safety profile in human studies, our study provides the rationale for evaluating TTP488 in clinical trials to treat or prevent metastatic TNBC.

01 Jun 2023·European journal of pharmacology

Azeliragon inhibits PAK1 and enhances the therapeutic efficacy of AKT inhibitors in pancreatic cancer

Article

Author: Kong, Weikang ; Cai, Xueting ; Chen, Jiao ; Zhang, Chunli ; Li, Tian ; Hu, Chunping ; Zhu, Lingxia ; Sun, Xiaoyan ; Ji, Wenjing ; Fan, Bo ; Cao, Peng

Pancreatic cancer is a lethal malignancy for which there is currently no effective treatment strategy. We previously reported that p21-activated kinase 1 (PAK1) is aberrantly expressed in pancreatic cancer patients and that targeted inhibition of PAK1 significantly suppressed pancreatic cancer progression in vitro and in vivo. In this study, we identified the drug azeliragon as a novel inhibitor of PAK1. Cell experiments revealed that azeliragon abolished PAK1 activation and promoted apoptosis in pancreatic cancer cells. Azeliragon was also found to significantly inhibit tumor growth in a pancreatic cancer xenograft model; when combined with afuresertib, an oral pan-AKT kinase inhibitor, azeliragon exhibited a strong synergistic effect against pancreatic cancer cells. Interestingly, afuresertib enhanced the antitumor efficacy of azeliragon in a xenograft mouse model. Collectively, our findings revealed previously unreported aspects of the drug azeliragon, and identified a novel combination strategy for the treatment of pancreatic cancer patients.

09 Apr 2023·Biomedicines

RAGE Inhibitors in Neurodegenerative Diseases.

Review

Author: Soni, Pallavi ; Reddy, V. Prakash ; Aryal, Puspa

Nonenzymatic reactions of reducing sugars with primary amino groups of amino acids, proteins, and nucleic acids, followed by oxidative degradations would lead to the formation of advanced glycation endproducts (AGEs). The AGEs exert multifactorial effects on cell damage leading to the onset of neurological disorders. The interaction of AGEs with the receptors for advanced glycation endproducts (RAGE) contribute to the activation of intracellular signaling and the expression of the pro-inflammatory transcription factors and various inflammatory cytokines. This inflammatory signaling cascade is associated with various neurological diseases, including Alzheimer's disease (AD), secondary effects of traumatic brain injury (TBI), amyotrophic lateral sclerosis (ALS), and diabetic neuropathy, and other AGE-related diseases, including diabetes and atherosclerosis. Furthermore, the imbalance of gut microbiota and intestinal inflammation are also associated with endothelial dysfunction, disrupted blood-brain barrier (BBB) and thereby the onset and progression of AD and other neurological diseases. AGEs and RAGE play an important role in altering the gut microbiota composition and thereby increase the gut permeability and affect the modulation of the immune-related cytokines. The inhibition of the AGE-RAGE interactions, through small molecule-based therapeutics, prevents the inflammatory cascade of events associated with AGE-RAGE interactions, and thereby attenuates the disease progression. Some of the RAGE antagonists, such as Azeliragon, are currently in clinical development for treating neurological diseases, including AD, although currently there have been no FDA-approved therapeutics based on the RAGE antagonists. This review outlines the AGE-RAGE interactions as a leading cause of the onset of neurological diseases and the current efforts on developing therapeutics for neurological diseases based on the RAGE antagonists.

News (Medical) associated with Azeliragon

28 May 2024

·www.prnewswire.com

CANTEX PHARMACEUTICALS ANNOUNCES FOUR ABSTRACTS TO BE PRESENTED FEATURING AZELIRAGON AT 2024 ASCO ANNUAL MEETING

WESTON, Fla., May 28, 2024 /PRNewswire/ -- Cantex Pharmaceuticals, Inc., a clinical stage pharmaceutical company focused on developing transformative therapies for cancer and other life-threatening medical conditions for which new treatments are urgently needed, announced today that Cantex's azeliragon, a well-tolerated once-a-day pill that inhibits "RAGE" (the receptor for advanced glycation end products), will be featured in four abstracts at this year's 2024 ASCO Annual Meeting to be held in Chicago. "The 2024 ASCO Annual Meeting represents an important opportunity to meet with the leading oncology researchers from around the world and showcase the progress of azeliragon clinical investigations at leading cancer centers in several difficult-to-treat cancers," said Stephen G. Marcus, M.D., Cantex's Chief Executive Officer. 2024 ASCO Annual Meeting Abstracts: Title: A phase I/II open label study to assess safety and preliminary evidence of a therapeutic effect of azeliragon in patients refractory to first-line treatment of metastatic pancreatic cancer. Abstract #: TPS4212 Title: Azeliragon, a RAGE inhibitor, in combination with temozolomide and radiotherapy in patients with newly diagnosed glioblastoma: Phase Ib/II CAN-201 NDG trial design. Abstract #: TPS2096 Title: RAGE inhibition to decrease cancer therapy related cardiotoxicity in women with early breast cancer (RAGE). Abstract #: TPS619 Title: A phase I/II study to assess safety and preliminary evidence of a therapeutic effect of azeliragon combined with stereotactic radiation therapy in patients with brain metastases (ADORATION). Abstract #: TPS2093 About Azeliragon Azeliragon is an orally administered capsule, taken once daily, that inhibits interactions of the receptor for advanced glycation end products (known as RAGE) with certain ligands, including HMGB1 and S100 proteins in the tumor microenvironment. Azeliragon was discovered by and originally under development for Alzheimer's disease by vTv Therapeutics Inc. (NASDAQ: VTVT) from which Cantex licensed worldwide rights to azeliragon. Clinical safety data from these trials, involving more than 2000 individuals dosed for periods up to 18 months, indicate that azeliragon is very well tolerated. Cantex has ongoing Phase II clinical trials in pancreatic cancer, glioblastoma, brain metastasis, breast cancer, and a Phase 3 trial in hospitalized patients with pneumonia to prevent acute kidney injury. These trials are based on azeliragon's robust preclinical data as well as its extensive clinical safety information from randomized placebo-controlled clinical trials. Azeliragon has U.S. Food and Drug Administration (FDA) orphan drug designation for the treatment of pancreatic cancer and glioblastoma. FDA Orphan Drug Designation provides Cantex with seven years of azeliragon marketing exclusivity from the time of product launch for the orphan indication, and several other important benefits, including assistance in the drug development process, tax credits for clinical costs, and exemptions from certain FDA fees. About Cantex Pharmaceuticals, Inc. Cantex Pharmaceuticals, Inc. is a privately held, clinical stage pharmaceutical company focused on developing transformative therapies for cancer and other life-threatening medical conditions for which new treatments are urgently needed. To learn more please visit . About vTv Therapeutics Inc. vTv Therapeutics Inc. is a clinical stage biopharmaceutical company focused on developing oral, small molecule drug candidates, led by cadisegliatin (TTP399), a potentially transformative treatment for the reduction of hypoglycemic episodes in type 1 diabetes patients. To learn more please visit vtvtherapeutics.com . Contact Information: Cantex Pharmaceuticals, Inc. Stephen G. Marcus, M.D. +1 954-315-3660 [email protected] Juan F. Rodriguez +1 954-315-3660 [email protected] Tiberend Strategic Advisors, Inc. Investors Daniel Kontoh-Boateng +1 862-213-1398 [email protected] Media Casey McDonald +1 646-577-8520 [email protected] SOURCE Cantex Pharmaceuticals, Inc.

Phase 2Orphan DrugPhase 3

20 May 2024

·www.prnewswire.com

CANTEX PHARMACEUTICALS RECEIVES FDA ORPHAN DRUG DESIGNATION FOR AZELIRAGON FOR THE TREATMENT OF PANCREATIC CANCER

WESTON, Fla., May 20, 2024 /PRNewswire/ -- Cantex Pharmaceuticals, Inc., a clinical-stage pharmaceutical company focused on developing transformative therapies for cancer and other life-threatening medical conditions for which new treatments are urgently needed, announced today that the U.S. Food and Drug Administration (FDA) has granted Orphan Drug Designation to Cantex' azeliragon, a well-tolerated once-a-day pill, for the treatment of pancreatic cancer. This new azeliragon orphan drug designation adds to azeliragon's previous orphan drug designation for the treatment of glioblastoma, received in early 2023. Pancreatic cancer, unless controlled at its earliest stages, often spreads to local tissues and to distant organs. Although surgery can be curative if pancreatic cancer is diagnosed at its very earliest stages, once the cancer has spread to distant organs, the current treatment has some, although limited, efficacy. New treatments are clearly needed. Cantex has an ongoing clinical trial studying the safety and efficacy of azeliragon in patients refractory to first-line treatment of metastatic pancreatic cancer. This clinical trial is enrolling metastatic pancreatic cancer patients in several world-class cancer treatment centers in the U.S. "Receiving FDA orphan drug status for azeliragon for the treatment of pancreatic cancer underscores the significant unmet need for novel treatment options for patients with pancreatic cancer, particularly for those patients with locally advanced, unresectable, or metastatic disease," commented Stephen G. Marcus, M.D., Chief Executive Officer of Cantex. "This designation strengthens our continued commitment to developing new azeliragon treatment options for patients with pancreatic cancer, as well as for other cancers and their complications, including glioblastoma, brain metastasis and breast cancer." FDA Orphan Drug Designation provides Cantex with seven years of azeliragon marketing exclusivity from the time of product launch for the orphan indication, and several other important benefits, including assistance in the drug development process, tax credits for clinical costs, and exemptions from certain FDA fees. About Azeliragon Azeliragon is an orally administered capsule, taken once daily, that inhibits interactions of the receptor for advanced glycation end products (known as RAGE) with certain ligands, including HMGB1 and S100 proteins in the tumor microenvironment. Azeliragon was discovered by and originally under development for Alzheimer's disease by vTv Therapeutics Inc. (NASDAQ: VTVT) from which Cantex licensed worldwide rights to azeliragon. Clinical safety data from these trials, involving more than 2000 individuals dosed for periods up to 18 months, indicate that azeliragon is very well tolerated. Cantex has ongoing Phase 2 clinical trials in pancreatic cancer, glioblastoma, brain metastasis, breast cancer, and a Phase 3 trial in hospitalized patients with pneumonia. These trials are based on azeliragon's robust preclinical data as well as its extensive clinical safety information from randomized placebo-controlled clinical trials. About Cantex Pharmaceuticals, Inc. Cantex Pharmaceuticals, Inc. is a privately held, clinical stage pharmaceutical company focused on developing transformative therapies for cancer and other life-threatening medical conditions for which new treatments are urgently needed. For more information, please visit . About vTv Therapeutics Inc. vTv Therapeutics Inc. is a clinical stage biopharmaceutical company focused on developing oral, small molecule drug candidates, led by cadisegliatin (TTP399), a potentially transformative treatment for the reduction of hypoglycemic episodes in type 1 diabetes patients. To learn more please visit vtvtherapeutics.com . Contact Data: Cantex Pharmaceuticals, Inc. Stephen G. Marcus, M.D. +1 954-315-3660 [email protected] Juan F. Rodriguez +1 954-315-3660 [email protected] Tiberend Strategic Advisors, Inc. Investors Daniel Kontoh-Boateng +1 862-213-1398 [email protected] Media Casey McDonald +1 646-577-8520 [email protected] SOURCE Cantex Pharmaceuticals, Inc.

Phase 2Orphan DrugPhase 3

19 Mar 2024

·www.biospace.com

CANTEX PHARMACEUTICALS TO PRESENT AT 5TH ANNUAL GLIOBLASTOMA DRUG DEVELOPMENT SUMMIT

Podium presentation will include clinical updates from the Company's Phase 2 clinical trials investigating azeliragon, in combination with radiation therapy with or without temozolomide, in newly diagnosed glioblastoma WESTON, Fla., March 19, 2024 /PRNewswire/ -- Cantex Pharmaceuticals, Inc., a clinical stage pharmaceutical company focused on developing transformative therapies for cancer and other life-threatening medical conditions for which new treatments are urgently needed, announced today that the Company's CEO, Stephen Marcus, M.D., will be an expert speaker at 5th Annual Glioblastoma Drug Development Summit, which will be held March 26-28 at the Hilton Boston Logan Airport. In a podium presentation titled, "Delving into a Clinical Update on Azeliragon for GBM - Implementable Lessons for Small Molecule Success," Dr. Marcus will update the Company's progress with its two ongoing azeliragon Phase 2 clinical trials. In those clinical trials, azeliragon is being studied in combination with radiation therapy with or without temozolomide in patients with newly diagnosed glioblastoma (GBM). In addition, Dr. Marcus will also highlight azeliragon's potential effect on cerebral edema and its potential ability to reduce dexamethasone dosing in GBM treatment. GBM is a highly malignant primary brain tumor for which current therapeutic options provide a limited life extension benefit. In 2023, Cantex received Food and Drug Administration Orphan Drug Designation for azeliragon for the treatment of glioblastoma. FDA Orphan Drug Designation provides Cantex with seven years of azeliragon marketing exclusivity from the time of product launch for the orphan indication, and several other important benefits, including assistance in the drug development process, tax credits for clinical costs, and exemptions from certain FDA fees. "We look forward to meeting with esteemed colleagues and researchers to discuss the many important advances being made to combat this challenging and devastating form of cancer and azeliragon's progress in our two Phase 2 GBM clinical trials," said Dr. Marcus. "We are excited to discuss this novel clinical candidate and its unique mechanism of action, which we believe has the potential to impact several devastating cancers that continue to challenge researchers, oncologists, and patients." Details of the event are as follows: During the conference, Dr. Marcus will conduct one-on-one meetings to review the Company's business and clinical development strategy, recent corporate achievements, and upcoming milestones. About Azeliragon Azeliragon is an orally administered capsule, taken once daily, that inhibits interactions of the receptor for advanced glycation end products (known as RAGE) with certain ligands, including HMGB1 and S100 proteins in the tumor microenvironment. Azeliragon was discovered by and originally under development for Alzheimer's disease by vTv Therapeutics Inc. (NASDAQ: VTVT) from which Cantex licensed worldwide rights to azeliragon. Clinical safety data from these trials, involving more than 2000 individuals dosed for periods up to 18 months, indicate that azeliragon is very well tolerated. Cantex has ongoing Phase 2 clinical trials in glioblastoma, brain metastasis, pancreatic cancer, breast cancer, and a Phase 3 trial in hospitalized patients with pneumonia to prevent acute kidney injury. These trials are based on azeliragon's robust preclinical data as well as its extensive clinical safety information from randomized placebo-controlled clinical trials. About Cantex Pharmaceuticals, Inc. Cantex Pharmaceuticals, Inc. is a privately held, clinical stage pharmaceutical company focused on developing transformative therapies for cancer and other life-threatening medical conditions for which new treatments are urgently needed. For more information, please visit . About vTv Therapeutics Inc. vTv Therapeutics Inc. is a clinical stage biopharmaceutical company focused on developing oral, small molecule drug candidates, led by cadisegliatin (TTP399), a potentially transformative treatment for the reduction of hypoglycemic episodes in type 1 diabetes patients. To learn more please visit vtvtherapeutics.com. Contact Information: Tiberend Strategic Advisors, Inc. Investors Daniel Kontoh-Boateng +1 862-213-1398 dboateng@tiberend.com Media Casey McDonald +1 646-577-8520 cmcdonald@tiberend.com Cantex Pharmaceuticals, Inc. Stephen G. Marcus, M.D. +1 954-315-3660 info@cantex.com Juan F. Rodriguez +1 954-315-3660 info@cantex.com Company Codes: NASDAQ-NMS:VTVT

Phase 2Orphan DrugRadiation Therapy

100 Deals associated with Azeliragon

External Link

KEGG	Wiki	ATC	Drug Bank
D11147	-	-	DB12689

R&D Status

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
COVID-19	Phase 3	US	Cantex Pharmaceuticals, Inc.	27 Sep 2023
Alzheimer Disease	Phase 3	US	vTv Therapeutics, Inc.	01 Apr 2015
Alzheimer Disease	Phase 3	AU	vTv Therapeutics, Inc.	01 Apr 2015
Alzheimer Disease	Phase 3	CA	vTv Therapeutics, Inc.	01 Apr 2015
Alzheimer Disease	Phase 3	IE	vTv Therapeutics, Inc.	01 Apr 2015
Alzheimer Disease	Phase 3	NZ	vTv Therapeutics, Inc.	01 Apr 2015
Alzheimer Disease	Phase 3	ZA	vTv Therapeutics, Inc.	01 Apr 2015
Alzheimer Disease	Phase 3	GB	vTv Therapeutics, Inc.	01 Apr 2015
Glioblastoma	Phase 2	ES	Cantex Pharmaceuticals, Inc.	05 Sep 2023
Pancreatic Cancer	Phase 2	-	Cantex Pharmaceuticals, Inc.	16 Jun 2023

Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT03980730 (CTgov)	Phase 2	Alzheimer Disease \| Glucose Intolerance	43	Azeliragon (Azeliragon)	pcdobwpdsj(ibtwczgbmv) = iajrhrtnbw enqgtqwmje (vejiltekvu, iutytxstpv - svbydgeyzf) View more	-	21 Jan 2022
				placebo (Placebo)	pcdobwpdsj(ibtwczgbmv) = ybwbhgrxcg enqgtqwmje (vejiltekvu, pzoiqyjknj - oqgkxrzhcc) View more
NCT02916056 (CTgov)	Phase 3	Alzheimer Disease	297	Azeliragon 5mg	tjyrssecra(dwjoopzhmu) = fbfxcgyhbb wsuuvhibzk (imjgcvmfyx, djbwwocdzv - npdbjudjkg) View more	-	01 Jun 2021
NCT02080364 (STEADFAST, CTgov)	Phase 3	Alzheimer Disease	880	Azeliragon (Azeliragon 5mg)	xzpnqmjrtu(oilwoprlqb) = nixurmarbk vnqmcykoxk (edvhsqjqhc, tyslgcystw - szmzfkdelg) View more	-	07 May 2021
				Placebo (Placebo)	xzpnqmjrtu(oilwoprlqb) = veiqnrpyre vnqmcykoxk (edvhsqjqhc, vxarkhktjn - vowausznnl) View more
NCT02080364 (STEADFAST, BusinessWire) Manual	Phase 3	Alzheimer Disease	800	Azeliragon	euqqasmtlc(mpcttpdtun) = vvklyndkzu sixzqmswcw (iscillvuxq ) View more	Negative	09 Apr 2018
				Placebo	euqqasmtlc(mpcttpdtun) = sywonocyok sixzqmswcw (iscillvuxq ) View more
AAIC2017	Not Applicable	-	-	Azeliragon 5 mg (fasted)	tdbkhusrbi(ymllzplklz) = vwszogmfxp pjvztvrcxe (xoeyaqmcem ) View more	-	01 Jul 2017
				Azeliragon 5 mg (fed)	tdbkhusrbi(ymllzplklz) = owgdguslij pjvztvrcxe (xoeyaqmcem ) View more
NCT00566397 (CTAD2015)	Phase 3	Alzheimer Disease	-	Azeliragon 20mg/day	yvcfjndggl(jdzmwvkrqn) = hmhfiegvjw wlutyuieei (flhwmqgzde, 6.6) View more	-	04 Nov 2015
				Azeliragon 5mg/day	yvcfjndggl(jdzmwvkrqn) = ftwrktpjgs wlutyuieei (flhwmqgzde, 5.4) View more

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