作者: Theodore W. Kurtz ; Stephen C. Benson ; Josef Meingassner ; Amar Chittiboyina ; Harrihar A. Pershadsingh ; Charles N. Ellis ; Meenakshi S. Venkatraman ; James Varani ; Christopher I. Ho ; Mitchell A. Avery

Novel thiazolidinedione derivatives of the potent antioxidant, alpha-lipoic (thioctic, 1,2-dithiolane) acid, were prepared. The prototype N-(2-[4-[2,4-dioxo(1,3-thiazolidin-5-yl)methyl]phenoxy]ethyl)-5-(1,2-dithiolan-3-yl)- N-methylpentanamide (designated BP-1003), and dithioester derivatives thereof were shown to be potent activators of peroxisome proliferator-activated receptor gamma (PPARgamma) (EC(50) range 15-101 nM) and modest activators of PPARalpha (EC(50) 5 microM). Both the relatively hydrophobic dithiolane prototype, BP-1003, and its water-soluble dithioglycinate derivative, BP-1017, were shown to inhibit the proliferation of human keratinocytes and suppress the production of interleukin-2 by human peripheral lymphocytes to a greater extent than the antidiabetic thiazolidinedione, rosiglitazone. Both oral and topical administration of BP-1017 showed significant antiinflammatory effects in the oxazolone-sensitized mouse model of allergic contact dermatitis (ACD). These findings suggest that water-soluble lipoic acid-based thiazolidinediones may be efficacious as oral and topical agents for treating inflammatory skin conditions such as contact dermatitis, atopic dermatitis, and psoriasis.

Biomedicines

BP1003 Decreases STAT3 Expression and Its Pro-Tumorigenic Functions in Solid Tumors and the Tumor Microenvironment

Article

作者: Roberts, Michael ; Dai, Bingbing ; Hooper, D. Craig ; Kean, Rhonda ; Fleming, Jason ; Ashizawa, Ana Tari ; Gagliardi, Maria ; Augustine, Jithesh Jose

Overexpression and aberrant activation of signal transducer and activator of transcription 3 (STAT3) contribute to tumorigenesis, drug resistance, and tumor-immune evasion, making it a potential cancer therapeutic target. BP1003 is a neutral liposome incorporated with a nuclease-resistant P-ethoxy antisense oligodeoxynucleotide (ASO) targeting the STAT3 mRNA. Its unique design enhances BP1003 stability, cellular uptake, and target affinity. BP1003 efficiently reduces STAT3 expression and enhances the sensitivity of breast cancer cells (HER2+, triple negative) and ovarian cancer cells (late stage, invasive ovarian cancer) to paclitaxel and 5-fluorouracil (5-FU) in both 2D and 3D cell cultures. Similarly, ex vivo and in vivo patient-derived models of pancreatic ductal adenocarcinoma (PDAC) show reduced tissue viability and tumor volume with BP1003 and gemcitabine combination treatments. In addition to directly affecting tumor cells, BP1003 can modulate the tumor microenvironment. Unlike M1 differentiation, monocyte differentiation into anti-inflammatory M2 macrophages is suppressed by BP1003, indicating its potential contribution to immunotherapy. The broad anti-tumor effect of BP1003 in numerous preclinical solid tumor models, such as breast, ovarian, and pancreatic cancer models shown in this work, makes it a promising cancer therapeutic.

项与 BP-1003 相关的新闻（医药）

2024-11-15

·GlobeNewswire-Health Care

Bio-Path Holdings Reports Third Quarter 2024 Financial Results

Expands DNAbilize® Technology Beyond Oncology into Obesity Conference Call to be Held Today at 8:30 A.M. ET HOUSTON, Nov. 15, 2024 (GLOBE NEWSWIRE) -- Bio-Path Holdings, Inc., (NASDAQ:BPTH), a biotechnology company leveraging its proprietary DNAbilize® antisense RNAi nanoparticle technology to develop a portfolio of targeted nucleic acid cancer drugs, today announced its financial results for the third quarter ended September 30, 2024 and provided an update on recent corporate developments. “The third quarter was a particularly productive period for Bio-Path as we initiated our obesity program, which marks the first application of our DNAbilize® platform beyond oncology and highlights its broad therapeutic potential," said Peter Nielsen, President and Chief Executive Officer of Bio-Path Holdings. "Importantly, we continued to advance our oncology programs and were delighted with the swift enrollment of the third cohort in our Phase 1/1b clinical trial of BP1002 in venetoclax-resistant AML patients, which was ahead of our projected timelines. We also published an article highlighting the broad anti-tumor effect of BP1003 in numerous preclinical solid tumor models, including breast, ovarian, and pancreatic cancer, in the peer-reviewed journal, Biomedicines." Recent Corporate Highlights Initiated BP1001-A Therapeutic Program for Treatment of Obesity. In October, the Company announced the initiation of a therapeutic program to develop BP1001-A for the treatment of obesity and related metabolic diseases. This program marks the first application of DNAbilize® technology for development of a non-cancer application, which highlights the broad therapeutic potential of this technology. The disease pathology leading to obesity suggests that BP1001-A, which suppresses the adaptor protein Grb2, has the potential to treat insulin resistance, a major contributor to obesity, Type 2 diabetes and other related metabolic diseases. Bio-Path expects downregulating Grb2 expression with BP1001-A will enhance insulin sensitivity.Completion of Enrollment for Third Dosing Cohort of Phase 1/1b Clinical Trial of BP1002 in Venetoclax-Resistant Acute Myeloid Leukemia (AML) Patients. In October, Bio-Path announced completion of enrollment for the third dosing cohort of the Company’s Phase 1/1b trial of BP1002 in venetoclax-resistant AML patients. The cohort enrolled more quickly than projected, which underscores the ongoing need for new treatment options for these relapsed/refractory patients.Publication in Peer-Reviewed Journal, Biomedicines. In September, Bio-Path published an article highlighting the therapeutic potential of BP1003 in a variety of cancer types in the peer-reviewed journal, Biomedicines. The article describes the broad anti-tumor effect of BP1003 in numerous preclinical solid tumor models including breast, ovarian, and pancreatic cancer. BP1003 is a neutral liposome incorporated with a nuclease resistant P-ethoxy antisense oligodeoxynucleotide targeting the STAT3 mRNA and its unique design enhances stability, cellular uptake, and target affinity.Reported Solid Tumor Patient Response Supporting BP1001-A’s Compelling Potential as Treatment for Advanced Solid Tumors. Bio-Path’s first patient in the second dose cohort in its Phase 1/1b advanced solid tumor clinical trial experiencing a positive response may signal that this analog of prexigebersen has potential as a new treatment for advanced solid tumors. The patient appears to be doing well on study after failing extensive chemotherapy and surgical treatment for gynecologic cancer, demonstrating a 15% reduction in her primary tumor through six cycles of treatment. Moreover, it appears that these positive outcomes may have contributed to allow her to continue with rigorous exercise and improved quality of life.The dose finding portion of the Phase 1/1b trial is comprised of BP1001-A monotherapy with no accompanying chemotherapy. This clinical trial of BP1001-A in patients with advanced or recurrent solid tumors has successfully completed the initial prescribed dose in the first cohort of 60 mg/m2 and began enrollment in the higher dose cohort of 90 mg/m2. The Phase 1b portion of the study is expected to commence after completion of three planned BP1001-A monotherapy dose level cohorts and is intended to assess the safety and efficacy of BP1001-A in combination with paclitaxel in patients with recurrent ovarian or endometrial tumors. Phase 1b studies are also expected to be opened in combination with gemcitabine in late-stage pancreatic cancer. Closed $4.0 Million Private Placement. In October, Bio-Path announced closing of a private placement priced at-the-market under Nasdaq rules for the issuance and sale of an aggregate of 4,597,702 shares of its common stock (or common stock equivalents in lieu thereof), series A warrants to purchase up to 6,407,657 shares of common stock and short-term series B warrants to purchase up to 6,407,657 shares of common stock at a purchase price of $0.87 per share of common stock (or per common stock equivalent in lieu thereof) and accompanying warrants in a private placement. The gross proceeds to the Company from the offering were approximately $4.0 million, before deducting the placement agent’s fees and other offering expenses payable by the Company, and excluding the proceeds, if any, from the exercise of the warrants. Financial Results for the Third Quarter Ended September 30, 2024 The Company reported a net loss of $2.1 million, or $0.70 per share, for the three months ended September 30, 2024, compared to a net loss of $3.2 million, or $6.36 per share, for the three months ended September 30, 2023.Research and development expense for the three months ended September 30, 2024 decreased to $1.3 million, compared to $2.3 million for the three months ended September 30, 2023 primarily due to decreased manufacturing expenses related to drug product releases as well as a decrease in expense related to our clinical trial for BP1001 in AML due to timing of patient enrollment during the quarter. General and administrative expense for the three months ended September 30, 2024 increased to $1.3 million, compared to $1.0 million for the three months ended September 30, 2023 primarily due to increased legal fees and salaries and benefits expense.As of September 30, 2024, the Company had cash of $0.6 million, compared to $1.1 million as of December 31, 2023. Net cash used in operating activities for the nine months ended September 30, 2024 was $7.7 million compared to $9.7 million for the comparable period in 2023. Net cash provided by financing activities for the nine months ended September 30, 2024 was $7.2 million. Conference Call and Webcast Information Bio-Path Holdings will host a conference call and webcast today at 8:30 a.m. ET to review these third quarter 2024 financial results and to provide a general update on the Company. To access the conference call please dial (844) 481-3014 (domestic) or (412) 317-1879 (international). A live audio webcast of the call and the archived webcast will be available in the Media section of the Company’s website at www.biopathholdings.com. About Bio-Path Holdings, Inc. Bio-Path is a biotechnology company developing DNAbilize®, a novel technology that has yielded a pipeline of RNAi nanoparticle drugs that can be administered with a simple intravenous transfusion. Bio-Path’s lead product candidate, prexigebersen (BP1001, targeting the Grb2 protein), is in a Phase 2 study for blood cancers, and BP1001-A, a drug product modification of prexigebersen, is in a Phase 1/1b study for solid tumors. The Company’s second product, BP1002, which targets the Bcl-2 protein, is being evaluated for the treatment of blood cancers and solid tumors, including lymphoma and acute myeloid leukemia. In addition, an IND is expected to be filed for BP1003, a novel liposome-incorporated STAT3 antisense oligodeoxynucleotide developed by Bio-Path as a specific inhibitor of STAT3. For more information, please visit the Company's website at www.biopathholdings.com. Forward-Looking Statements This press release contains forward-looking statements that are made pursuant to the safe harbor provisions of the federal securities laws. These statements are based on management's current expectations and accordingly are subject to uncertainty and changes in circumstances. Any express or implied statements contained in this press release that are not statements of historical fact may be deemed to be forward-looking statements. Any statements that are not historical facts contained in this release are forward-looking statements that involve risks and uncertainties, including Bio-Path’s ability to raise needed additional capital on a timely basis in order for it to continue its operations, have success in the clinical development of its technologies, the timing of enrollment and release of data in such clinical studies, the accuracy of such data, limited patient populations of early stage clinical studies and the possibility that results from later stage clinical trials with much larger patient populations may not be consistent with earlier stage clinical trials, the maintenance of intellectual property rights, that patents relating to existing or future patent applications will be issued or that any issued patents will provide meaningful protection of our drug candidates, the impact, risks and uncertainties related to global pandemics, including the COVID-19 pandemic, and actions taken by governmental authorities or others in connection therewith, and such other risks which are identified in Bio-Path's most recent Annual Report on Form 10-K, in any subsequent quarterly reports on Form 10-Q and in other reports that Bio-Path files with the Securities and Exchange Commission from time to time. These documents are available on request from Bio-Path Holdings or at www.sec.gov. Bio-Path disclaims any intention or obligation to update or revise any forward-looking statements, whether as a result of new information, future events or otherwise. Contact Information: Investors Will O’ConnorStern Investor Relations, Inc.212-362-1200will@sternir.com Doug Morris Investor Relations Bio-Path Holdings, Inc. 832-742-1369

临床2期临床1期财报

2024-11-08

·GlobeNewswire-Health Care

Bio-Path Holdings to Announce Third Quarter 2024 Financial Results on November 15, 2024

HOUSTON, Nov. 08, 2024 (GLOBE NEWSWIRE) -- Bio-Path Holdings, Inc., (NASDAQ: BPTH) a biotechnology company leveraging its proprietary DNAbilize® antisense RNAi nanoparticle technology to develop a portfolio of targeted nucleic acid cancer drugs, today announced that it will host a live conference call and audio webcast on Friday, November 15, 2024 at 8:30 a.m. ET to report financial results for the third quarter ended September 30, 2024 and to provide a business overview. To access the live conference call, please call (844) 481-3014 (domestic) or (412) 317-1879 (international) at least five minutes prior to the start time. A live audio webcast of the call will also be available on the Presentations section of the Company’s website, www.biopathholdings.com. An archived webcast will be available on the Bio-Path website approximately two hours after the event. About Bio-Path Holdings, Inc. Bio-Path is a biotechnology company developing DNAbilize®, a novel technology that has yielded a pipeline of RNAi nanoparticle drugs that can be administered with a simple intravenous transfusion. Bio-Path’s lead product candidate, prexigebersen (BP1001, targeting the Grb2 protein), is in a Phase 2 study for blood cancers, and BP1001-A, a drug product modification of prexigebersen, is in a Phase 1/1b study for solid tumors. The Company’s second product, BP1002, which targets the Bcl-2 protein, is being evaluated for the treatment of blood cancers and solid tumors, including lymphoma and acute myeloid leukemia. In addition, an IND is expected to be filed for BP1003, a novel liposome-incorporated STAT3 antisense oligodeoxynucleotide developed by Bio-Path as a specific inhibitor of STAT3. For more information, please visit the Company's website at http://www.biopathholdings.com. Contact Information: Investors Will O’ConnorStern Investor Relations 212-362-1200will@sternir.com Doug Morris Investor Relations Bio-Path Holdings, Inc. 832-742-1369

临床2期财报临床1期

2024-10-10

·GlobeNewswire-Health Care

Bio-Path Holdings Announces Closing of $4.0 Million Private Placement Priced At-the-Market Under Nasdaq Rules

HOUSTON, Oct. 10, 2024 (GLOBE NEWSWIRE) -- Bio-Path Holdings, Inc. (NASDAQ:BPTH) (“Bio-Path” or the “Company”), a biotechnology company leveraging its proprietary DNAbilize® liposomal delivery and antisense technology to develop a portfolio of targeted nucleic acid cancer drugs, today announced that it has closed its previously announced private placement priced at-the-market under Nasdaq rules for the issuance and sale of an aggregate of 4,597,702 shares of its common stock (or common stock equivalents in lieu thereof), series A warrants to purchase up to 6,407,657 shares of common stock and short-term series B warrants to purchase up to 6,407,657 shares of common stock at a purchase price of $0.87 per share of common stock (or per common stock equivalent in lieu thereof) and accompanying warrants in a private placement. The series A warrants and short-term series B warrants have an exercise price of $1.00 per share and will be exercisable beginning on the effective date of stockholder approval of the issuance of the shares issuable upon exercise of the warrants (the “Stockholder Approval Date”). The series A warrants will expire five years from the Stockholder Approval Date and the short-term series B warrants will expire twenty-four months from the Stockholder Approval Date. H.C. Wainwright & Co. acted as the exclusive placement agent for the offering. The gross proceeds to the Company from the offering were approximately $4.0 million, before deducting the placement agent’s fees and other offering expenses payable by the Company, and excluding the proceeds, if any, from the exercise of the warrants. The Company currently intends to use the net proceeds from the offering for working capital and general corporate purposes. The securities described above were offered in a private placement under Section 4(a)(2) of the Securities Act of 1933, as amended (the “Securities Act”), and/or Regulation D promulgated thereunder and, along with the shares of common stock underlying the warrants, have not been registered under the Securities Act, or applicable state securities laws. Accordingly, the securities described above, including the shares of common stock underlying the warrants, may not be offered or sold in the United States except pursuant to an effective registration statement or an applicable exemption from the registration requirements of the Securities Act and such applicable state securities laws. In addition, effective on the closing of the private placement certain outstanding series A warrants to purchase up to an aggregate of 1,809,955 shares of the Company’s common stock and series B warrants to purchase up to an aggregate of 1,809,955 shares of the Company’s common stock issued in June 2024 were cancelled. This press release does not constitute an offer to sell or a solicitation of an offer to buy the securities in this offering, nor shall there be any sale of these securities in any state or other jurisdiction in which such offer, solicitation or sale would be unlawful prior to the registration or qualification under the securities laws of any such state or other jurisdiction. About Bio-Path Holdings, Inc. Bio-Path is a biotechnology company developing DNAbilize®, a novel technology that has yielded a pipeline of RNAi nanoparticle drugs that can be administered with a simple intravenous infusion. Bio-Path’s lead product candidate, prexigebersen (BP1001, targeting the Grb2 protein), is in a Phase 2 study for blood cancers, and BP1001-A, a drug product modification of prexigebersen, is in a Phase 1/1b study for solid tumors. The Company’s second product, BP1002, which targets the Bcl-2 protein, is being evaluated for the treatment of blood cancers and solid tumors, including lymphoma and acute myeloid leukemia. In addition, an IND application is expected to be filed for BP1003, a novel liposome-incorporated STAT3 antisense oligodeoxynucleotide developed by Bio-Path as a specific inhibitor of STAT3. For more information, please visit the Company's website at www.biopathholdings.com. Forward-Looking Statements This press release contains forward-looking statements that are made pursuant to the safe harbor provisions of the federal securities laws, including statements related to the intended use of proceeds from the private placement. These statements are based on management's current expectations and accordingly are subject to uncertainty and changes in circumstances. Any express or implied statements contained in this press release that are not statements of historical fact may be deemed to be forward-looking statements. Any statements that are not historical facts contained in this release are forward-looking statements that involve risks and uncertainties, including market and other conditions, Bio-Path’s ability to regain and maintain compliance with Nasdaq’s continued listing requirements, Bio-Path’s ability to raise needed additional capital on a timely basis in order for it to continue its operations, have success in the clinical development of its technologies, the timing of enrollment and release of data in such clinical studies, the accuracy of such data, limited patient populations of early stage clinical studies and the possibility that results from later stage clinical trials with much larger patient populations may not be consistent with earlier stage clinical trials, the maintenance of intellectual property rights, that patents relating to existing or future patent applications will be issued or that any issued patents will provide meaningful protection of our drug candidates, the impact, risks and uncertainties related to global pandemics, including the COVID-19 pandemic, and actions taken by governmental authorities or others in connection therewith, and such other risks which are identified in Bio-Path's most recent Annual Report on Form 10-K, in any subsequent quarterly reports on Form 10-Q and in other reports that Bio-Path files with the Securities and Exchange Commission from time to time. These documents are available on request from Bio-Path or at www.sec.gov. Bio-Path disclaims any intention or obligation to update or revise any forward-looking statements, whether as a result of new information, future events or otherwise. Contact Information: Investors Will O’ConnorStern Investor Relations, Inc.212-362-1200will@sternir.com Doug MorrisInvestor RelationsBio-Path Holdings, Inc.832-742-1369

临床2期

100 项与 BP-1003 相关的药物交易

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