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Cambridge, MA, November 7, 2025 — Flare Therapeutics Inc. (FlareTx), a clinical-stage biotechnology company targeting transcription factors to discover precision medicines for oncology and other therapeutic areas, today announced the presentation of a correlative biomarker analysis from the Phase 1A clinical study of FX-909, a first-in-class orally available small molecule inhibitor of peroxisome proliferator-activated receptor gamma (PPARG), the master regulator of the luminal lineage, in locally-advanced or metastatic urothelial cancer (UC). This analysis includes novel insights regarding FX-909’s immune modulatory mechanism of action and demonstrate that FX-909 exerts immune-modulatory activity as a single agent, supporting the rationale for combination with an anti-PD-1 inhibitor in advanced UC.
Matthew L. Milowsky, M.D., Lineberger Comprehensive Cancer Center, University of North Carolina, Chapel Hill, will present these results in a poster presentation titled “Phase 1 Clinical Data Show FX-909, a First-in-Class Oral PPARG Inhibitor, Drives Immune Modulation and Pro-Inflammatory Cytokine Induction in IO-Experienced Patients with Advanced Urothelial Carcinoma” on Saturday, November 8, 2025 from 10:00 a.m. to 6:35 p.m. ET at the Society for Immunotherapy of Cancer (SITC) 2025 40th Anniversary Annual Meeting in National Harbor, MD.
“Along with the recently presented clinical activity data for FX-909, it is particularly exciting to now present this correlative data showing the induction of pro-inflammatory cytokines and chemokines and the promotion of T-cell expansion. This analysis supports PPARG inhibition as a potential strategy to overcome immune resistance and provides a rationale for the planned cohort evaluating FX-909 in combination with pembrolizumab. I look forward to seeing this cohort initiate early in 2026,” commented Dr. Milowsky.
“Having recently disclosed that FX-909 has achieved clinical proof of concept as a monotherapy, we are very pleased to now share IO-experienced patient level evidence that support our translational hypothesis regarding the immune modulatory mechanism of action of FX-909. We look forward to generating data from our planned cohort of FX-909 in combination with pembrolizumab and believe this approach could provide a “one-two punch” to overcome IO resistance,” said Michaela Bowden, Ph.D., Chief Development Officer of Flare Therapeutics.
Phase 1A Study
Correlative biomarker evaluations were conducted on a subset of IO-experienced advanced UC patients enrolled in the Phase 1A open-label 3+3 dose-escalation study. This analysis evaluated baseline molecular features of archival tumors and longitudinal proteomic and single-cell immune profiles to elucidate the immune-modulatory mechanism of FX-909.
Key highlights include:
Taken together these results demonstrate that FX-909 exerts immune modulatory activity as a single agent supporting the rationale for combination with an anti-PD-1 inhibitor in advanced urothelial carcinoma.
FX-909 Next Steps
FX-909 is currently being evaluated in a Phase 1B expansion study evaluating safety and efficacy in second line or beyond to determine the recommended Phase 2 dose in a biomarker-defined PPARGhigh locally advanced (unresectable) or metastatic UC patient population. The Phase 1 Part B study adopts a randomized 2-stage design. A validated immunohistochemistry (IHC)-based test has been developed to identify patients eligible for enrollment in the expansion study. The company expects interim efficacy data in a biomarker-defined population at the recommended Phase 2 dose in the first quarter of 2026.
In the first quarter of 2026, the company expects to initiate enrollment of a Phase 1 combination cohort that will investigate the safety, tolerability, immunologic effects and preliminary efficacy of escalating doses of FX-909 in combination with standard dose KEYTRUDA® (pembrolizumab) in patients with advanced urothelial carcinoma. As announced on October 21, 2025, Merck (known as MSD outside of the United States and Canada) has agreed to provide its anti-PD-1 therapy KEYTRUDA for this combination cohort under the clinical trial collaboration and supply agreement.
More information about the trial is available at clinicaltrials.gov using the identifier NCT05929235.
About Advanced Urothelial Cancer
Advanced urothelial cancer (UC) is an aggressive and challenging form of bladder cancer, representing approximately 25% of all bladder cancers diagnosed each year. In the United States, bladder cancer accounts for approximately 84,000 new cases each year, with urothelial carcinoma being the predominant histologic type. In advanced or metastatic stages, the disease is notably difficult to treat, with over 50% of patients experiencing disease progression within six to nine months of first-line chemotherapy. The five-year survival rate for metastatic UC remains poor, with estimates below 6%. While the introduction of checkpoint inhibitors and targeted therapies has expanded treatment options, clinical outcomes remain suboptimal, underscoring an urgent need for additional and more effective treatment options. Molecular subtyping has revealed that luminal tumors, or tumors that are characterized by high PPARG expression, comprise approximately 65% of advanced urothelial cancers. These luminal tumors are often or invariably characterized by activation of the PPARG (peroxisome proliferator-activated receptor gamma) pathway, which plays a critical role in maintaining tumor identity, promoting tumor growth, and contributing to immune evasion. Novel approaches such as PPARG inhibition are emerging as promising strategies to improve outcomes for patients that have UC with high PPARG expression. It is estimated that the United States alone, there are approximately 14,000 new cases of advanced urothelial cancer with high PPARG expression diagnosed each year, based on the portion of luminal subtypes and overall incidence data.
About Flare Therapeutics Inc.
Flare Therapeutics is a clinical-stage biotechnology company exclusively focused on drugging transcription factors to fully unlock the therapeutic potential of this previously elusive target class. The company’s lead program, FX-909, is a first-in-class orally available small molecule inhibitor of PPARG, the master regulator of the luminal lineage, that is initially being developed for locally advanced or metastatic urothelial cancer. FX-909 has achieved clinical proof-of-concept in a Phase 1A study as a monotherapy and is actively dosing patients in a Phase 1B to determine the recommended Phase 2 dose in a biomarker-defined population. The second lead program, FX-111, is a novel and highly differentiated potent and selective degrader for ARON, the transcriptionally active, hormone-bound androgen receptor. This approach offers the potential to overcome key vulnerabilities of conventional therapies that target AROFF and has broad potential across prostate cancer at all stages. FX-111 is undergoing Investigational New Drug (IND)-enabling studies for initial development for the treatment of metastatic castration-resistant prostate cancer (mCRPC). These two programs, along with an earlier-stage portfolio targeting transcription factors involved in oncology and other therapeutic areas, leverages Flare Therapeutics’ integrated discovery platform of capabilities that identifies novel validated ligands to the undrugged proteome. For more information, please visit www.flaretx.com and follow us on LinkedIn.
KEYTRUDA® is a registered trademark of Merck Sharp & Dohme LLC, a subsidiary of Merck & Co., Inc., Rahway, NJ, USA.
Contacts:
Investors:
Sarah McCabe
Media:
Timothy Cockroft
Cambridge, MA, November 3, 2025 — Flare Therapeutics Inc. (FlareTx), a clinical-stage biotechnology company targeting transcription factors to discover precision medicines for oncology and other therapeutic areas, today announced that company management will present at the following two healthcare conferences in November:
About Flare Therapeutics Inc.
Flare Therapeutics is a clinical-stage biotechnology company exclusively focused on drugging transcription factors to fully unlock the therapeutic potential of this previously elusive target class. The company’s lead program, FX-909, is a first-in-class orally available small molecule inhibitor of PPARG, the master regulator of the luminal lineage, that is initially being developed for locally advanced or metastatic urothelial cancer. FX-909 has achieved clinical proof-of-concept in a Phase 1A study as a monotherapy and is actively dosing patients in a Phase 1B to determine the recommended Phase 2 dose in a biomarker-defined population. The second lead program, FX-111, is a novel and highly differentiated potent and selective degrader for ARON, the transcriptionally active, hormone-bound androgen receptor. This approach offers the potential to overcome key vulnerabilities of conventional therapies that target AROFF and has broad potential across prostate cancer at all stages. FX-111 is undergoing Investigational New Drug (IND)-enabling studies for initial development for the treatment of metastatic castration-resistant prostate cancer (mCRPC). These two programs, along with an earlier-stage portfolio targeting transcription factors involved in oncology and other therapeutic areas, leverage Flare Therapeutics’ integrated discovery platform of capabilities that identifies novel validated ligands to the undrugged proteome. For more information, please visit www.flaretx.com and follow us on LinkedIn.
Contacts:
Investors:
Sarah McCabe
Media:
Timothy Cockroft
Cambridge, MA, October 30, 2025 — Flare Therapeutics Inc. (FlareTx), a clinical-stage biotechnology company targeting transcription factors to discover precision medicines for oncology and other therapeutic areas, today announced a poster presentation of the correlative biomarker analysis from the FX-909 Phase 1A clinical study at the upcoming Society for Immunotherapy of Cancer (SITC) 2025 40th Anniversary Annual Meeting being held November 5-9, 2025 in National Harbor, MD.
The presentation at SITC will build on the first disclosure of the part A data from the ongoing Phase 1 study for FX-909, which were recently presented at the AACR-NCI-EORTC International Conference, and include novel insights regarding FX-909’s immune modulatory mechanism of action. FX-909 is a first-in-class orally available small molecule inhibitor of peroxisome proliferator-activated receptor gamma (PPARG), the master regulator of the luminal lineage, currently in a Phase 1B study for the treatment of locally-advanced or metastatic urothelial cancer (UC).
SITC poster presentation details are as follows:
Abstract Title: Phase 1 Clinical Data Show FX-909, a First-in-Class Oral PPARG Inhibitor, Drives Immune Modulation and Pro-Inflammatory Cytokine Induction in IO-Experienced Patients with Advanced Urothelial Carcinoma
Abstract Number: 1318
Session: Exhibits & Poster Viewing
Presenter: Matthew L Milowsky
Date, Time: Saturday, November 8, 2025 from 10:00 a.m. to 6:35 p.m. ET
Location: Lower Level Atrium, Prince George’s ABC
About Flare Therapeutics Inc.
Flare Therapeutics is a clinical-stage biotechnology company exclusively focused on drugging transcription factors to fully unlock the therapeutic potential of this previously elusive target class. The company’s lead program, FX-909, is a first-in-class orally available small molecule inhibitor of PPARG, the master regulator of the luminal lineage, that is initially being developed for locally advanced or metastatic urothelial cancer. FX-909 has achieved clinical proof-of-concept in a Phase 1A study as a monotherapy and is actively dosing patients in a Phase 1B to determine the recommended Phase 2 dose in a biomarker-defined population. The second lead program, FX-111, is a novel and highly differentiated potent and selective degrader for ARON, the transcriptionally active, hormone-bound androgen receptor. This approach offers the potential to overcome key vulnerabilities of conventional therapies that target AROFF and has broad potential across prostate cancer at all stages. FX-111 is undergoing Investigational New Drug (IND)-enabling studies for initial development for the treatment of metastatic castration-resistant prostate cancer (mCRPC). These two programs, along with an earlier-stage portfolio targeting transcription factors involved in oncology and other therapeutic areas, leverages Flare Therapeutics’ integrated discovery platform of capabilities that identifies novel validated ligands to the undrugged proteome. For more information, please visit www.flaretx.com and follow us on LinkedIn.
Contacts:
Investors:
Sarah McCabe
Media:
Timothy Cockroft
Cambridge, MA, October 24, 2025 — Flare Therapeutics Inc. (FlareTx), a clinical-stage biotechnology company targeting transcription factors to discover precision medicines for oncology and other therapeutic areas, today announced part A data from the ongoing Phase 1 study of FX-909, a first-in-class orally available small molecule inhibitor of peroxisome proliferator-activated receptor gamma (PPARG), the master regulator of the luminal lineage, in locally-advanced or metastatic urothelial cancer (UC). FX-909 demonstrated early signs of clinical benefit in patients with advanced urothelial carcinoma as a monotherapy with a favorable safety profile.
Xin Gao, M.D., Medical Oncologist and Clinical Investigator, Massachusetts General Hospital, presented these results in an oral presentation titled “Safety and clinical activity of FX-909, a first-in-class oral small molecule inhibitor of peroxisome proliferator-activated receptor gamma (PPARG), a master regulator of luminal lineage in patients with advanced urothelial carcinoma” today at the AACR-NCI-EORTC International Conference on Molecular Targets and Cancer Therapeutics.
“These preliminary data show a first-in-mechanism drug with promising single agent efficacy at all doses evaluated in a heavily pre-treated locally advanced and metastatic UC patient population. I believe this clinical proof-of-concept supports further development of FX-909. In the ongoing Phase 1B study, patients are being prospectively screened for high expression of PPARG, the hallmark of the luminal lineage, which accounts for approximately 65% of cases of advanced UC. I look forward to seeing the clinical activity data in this biomarker defined population,” commented Dr. Gao.
“In the last decade, the advanced UC treatment landscape has evolved significantly, and the standard of care paradigm has changed. However, despite these advances, there is still a large unmet need for efficacious treatments with better tolerability and durability in this difficult-to-treat patient population. We are encouraged by the preliminary clinical efficacy we are seeing for FX-909 and are focused on executing the ongoing Phase 1B study that will deliver data for our novel PPARG inhibitor in a biomarker-defined population of UC patients. We believe FX-909 may represent a significant step toward addressing the disease at its source by directly targeting the cell of origin and addressing the underlying disease biology, and we are eager to continue exploring the full potential of this agent,” remarked Dr. Michael L. Meyers, Chief Medical Officer at Flare Therapeutics.
Phase 1A Study
The Phase 1A open-label 3+3 dose-escalation study evaluated the safety, tolerability, pharmacokinetics, pharmacodynamics, and preliminary clinical activity of FX-909 administered orally once daily (QD) in 28-day cycles and enrolled patients with advanced solid malignancies, including advanced UC. Data for 46 patients, including 36 patients with advanced UC, who were treated across four dose levels; 30 mg (12); 50 mg (15); 70 mg (13); and 100 mg (6) were reported as of September 17, 2025.
Key data highlights include:
Based on the totality of the Part A data, 30 mg and 50 mg QD doses were selected for further optimization. Prospective pre-screening to select for patients with a Tumor Proportional Score (TPS) cutoff of ³60%, newly defined as PPARGhigh, is being implemented in the Phase 1 Part B study.
FX-909 Next Steps
FX-909 is currently being evaluated in a Phase 1B expansion study evaluating safety and efficacy in second line or beyond to determine the recommended Phase 2 dose in a biomarker-defined PPARGhigh locally advanced (unresectable) or metastatic UC patient population. The Phase 1 Part B study adopts a randomized 2-stage design. A validated immunohistochemistry (IHC)-based test has been developed to identify patients eligible for enrollment in the expansion study. The company expects interim efficacy data in a biomarker-defined population at the recommended Phase 2 dose in the first quarter of 2026. More information about the trial is available at clinicaltrials.gov using the identifier NCT05929235.
Webinar Information
An on-demand webinar with company management and investigators, Xin Gao, M.D. and Matthew Galsky, M.D., reviewing this data is now available on the Flare Therapeutics website and can also be accessed here: https://edge.media-server.com/mmc/p/wbj4uhqp. The poster presentation is also available on the Flare Therapeutics website under presentations & publications.
About Advanced Urothelial Cancer
Advanced urothelial cancer (UC) is an aggressive and challenging form of bladder cancer, representing approximately 25% of all bladder cancers diagnosed each year. In the United States, bladder cancer accounts for approximately 84,000 new cases each year, with urothelial carcinoma being the predominant histologic type. In advanced or metastatic stages, the disease is notably difficult to treat, with over 50% of patients experiencing disease progression within six to nine months of first-line chemotherapy. The five-year survival rate for metastatic UC remains poor, with estimates below 6%. While the introduction of checkpoint inhibitors and targeted therapies has expanded treatment options, clinical outcomes remain suboptimal, underscoring an urgent need for additional and more effective treatment options. Molecular subtyping has revealed that luminal tumors, or tumors that are characterized by high PPARG expression, comprise approximately 65% of advanced urothelial cancers. These luminal tumors are often or invariably characterized by activation of the PPARG (peroxisome proliferator-activated receptor gamma) pathway, which plays a critical role in maintaining tumor identity, promoting tumor growth, and contributing to immune evasion. Novel approaches such as PPARG inhibition are emerging as promising strategies to improve outcomes for patients that have UC with high PPARG expression. It is estimated that in the United States alone, there are approximately 14,000 new cases of advanced urothelial cancer with high PPARG expression diagnosed each year, based on the portion of luminal subtypes and overall incidence data.
About Flare Therapeutics Inc.
Flare Therapeutics is a clinical-stage biotechnology company exclusively focused on drugging transcription factors to fully unlock the therapeutic potential of this previously elusive target class. The company’s lead program, FX-909, is a first-in-class orally available small molecule inhibitor of PPARG, the master regulator of the luminal lineage, that is initially being developed for locally advanced or metastatic urothelial cancer. FX-909 has achieved clinical proof-of-concept in a Phase 1A study as a monotherapy and is actively dosing patients in a Phase 1B to determine the recommended Phase 2 dose in a biomarker-defined population. The second lead program, FX-111, is a novel and highly differentiated potent and selective degrader for ARON, the transcriptionally active, hormone-bound androgen receptor. This approach offers the potential to overcome key vulnerabilities of conventional therapies that target AROFF and has broad potential across prostate cancer at all stages. FX-111 is undergoing Investigational New Drug (IND)-enabling studies for initial development for the treatment of metastatic castration-resistant prostate cancer (mCRPC). These two programs, along with an earlier-stage portfolio targeting transcription factors involved in oncology and other therapeutic areas, leverage Flare Therapeutics’ integrated discovery platform of capabilities that identifies novel validated ligands to the undrugged proteome. For more information, please visit www.flaretx.com and follow us on LinkedIn.
Contacts:
Investors:
Sarah McCabe
Media:
Timothy Cockroft
Cambridge, MA, October 21, 2025 — Flare Therapeutics Inc. (FlareTx), a clinical-stage biotechnology company targeting transcription factors to discover precision medicines for oncology and other therapeutic areas, today announced that it has entered into a clinical trial collaboration and supply agreement with Merck (known as MSD outside of the United States and Canada). FX-909, a first-in-class orally available small molecule inhibitor of PPARG, the master regulator of the luminal lineage, will be evaluated in combination with KEYTRUDA® (pembrolizumab), Merck’s anti-PD-1 (programmed cell death receptor-1) therapy, in a new cohort within the company’s ongoing Phase 1 study in locally-advanced or metastatic urothelial cancer (UC).
“FX-909 has achieved clinical proof of concept in the Phase 1A trial as a monotherapy, and we are very pleased to announce this agreement with Merck to add a combination arm to our ongoing Phase 1 study,” said Michaela Bowden, PhD, Chief Development Officer. “FX-909 directly targets luminal cancer cells along with driving immune modulation, inducing pro-inflammatory signaling and T-cell expansion in circulation. Combining FX-909 with an anti-PD-1 may provide a one-two punch to overcome IO resistance, opening the door to first-line treatment for advanced UC, earlier stages of disease, and other solid tumors in which PPARG actively drives immune evasion.”
Under the terms of the supply agreement, Merck will provide its anti-PD-1 therapy KEYTRUDA to be used in combination with FX-909. The Phase 1 study combination cohort is expected to begin enrollment in the first quarter of 2026 and will investigate the safety, tolerability, immunologic effects and preliminary efficacy of escalating doses of FX-909 in combination with standard dose pembrolizumab in patients with advanced urothelial carcinoma.
About Flare Therapeutics Inc.
Flare Therapeutics is a clinical-stage biotechnology company exclusively focused on drugging transcription factors to fully unlock the therapeutic potential of this previously elusive target class. The company’s lead program, FX-909, is a first-in-class orally available small molecule inhibitor of PPARG, the master regulator of the luminal lineage, that is initially being developed for locally advanced or metastatic urothelial cancer. FX-909 has achieved clinical proof-of-concept in a Phase 1A study as a monotherapy and is actively dosing patients in a Phase 1B expansion study to determine the recommended Phase 2 dose in a biomarker-defined population. The second lead program, FX-111, is a novel and highly differentiated potent and selective degrader for ARON, the transcriptionally active, hormone-bound androgen receptor. This approach offers the potential to overcome key vulnerabilities of conventional therapies that target AROFF and has broad potential across prostate cancer at all stages. FX-111 is undergoing Investigational New Drug (IND)-enabling studies for initial development for the treatment of metastatic castration-resistant prostate cancer (mCRPC). These two programs, along with an earlier-stage portfolio targeting transcription factors involved in oncology and other therapeutic areas, leverage Flare Therapeutics’ integrated discovery platform of capabilities that identifies novel validated ligands to the undrugged proteome. For more information, please visit www.flaretx.com and follow us on LinkedIn.
KEYTRUDA® is a registered trademark of Merck Sharp & Dohme LLC, a subsidiary of Merck & Co., Inc., Rahway, NJ, USA.
Contacts:
Investors:
Sarah McCabe
Media:
Timothy Cockroft
Cambridge, MA, October 14, 2025 — Flare Therapeutics Inc. (FlareTx), a clinical-stage biotechnology company targeting transcription factors to discover precision medicines for oncology and other therapeutic areas, today announced the presentation of FX-909 Phase 1A clinical data in an oral presentation at the upcoming AACR-NCI-EORTC International Conference on Molecular Targets and Cancer Therapeutics being held October 22-26, 2025 in Boston, MA. FX-909 is a first-in-class orally available small molecule inhibitor of peroxisome proliferator-activated receptor gamma (PPARG), the master regulator of the luminal lineage, currently in a Phase 1B study for the treatment of locally-advanced or metastatic urothelial cancer (UC).
AACR-NCI-EORTC oral presentation details are as follows:
Abstract Title: Safety and clinical activity of FX-909, a first-in-class oral small molecule inhibitor of peroxisome proliferator-activated receptor gamma (PPARG), a master regulator of luminal lineage in patients with advanced urothelial carcinoma
Session: Plenary Session 4: Clinical Trials Plenary Session
Presenter: Xin Gao
Date, Time: Friday, October 24, 2025 from 10:00 a.m. to 11:40 a.m. ET
Location: Level 3, Ballroom AB
About Flare Therapeutics Inc.
Flare Therapeutics is a clinical-stage biotechnology company exclusively focused on drugging transcription factors to fully unlock the therapeutic potential of this previously elusive target class. The company’s lead program, FX-909, is a first-in-class orally available small molecule inhibitor of PPARG, the master regulator of the luminal lineage, that is initially being developed for locally advanced or metastatic urothelial cancer. FX-909 has achieved clinical proof-of-concept in a Phase 1A study as a monotherapy and is actively dosing patients in a Phase 1B to determine the recommended Phase 2 dose in a biomarker-defined population. The second lead program, FX-111, is a novel and highly differentiated potent and selective degrader for ARON, the transcriptionally active, hormone-bound androgen receptor. This approach offers the potential to overcome key vulnerabilities of conventional therapies that target AROFF and has broad potential across prostate cancer at all stages. FX-111 is undergoing Investigational New Drug (IND)-enabling studies for initial development for the treatment of metastatic castration-resistant prostate cancer (mCRPC). These two programs, along with an earlier-stage portfolio targeting transcription factors involved in oncology and other therapeutic areas, leverage Flare Therapeutics’ integrated discovery platform of capabilities that identifies novel validated ligands to the undrugged proteome. For more information, please visit www.flaretx.com and follow us on LinkedIn.
Contacts:
Investors:
Sarah McCabe
Media:
Cambridge, MA, August 27, 2025 — Flare Therapeutics Inc. (FlareTx), a clinical-stage biotechnology company targeting transcription factors to discover precision medicines for oncology and other therapeutic areas, today announced that the company will participate in the following investor conferences in September:
About Flare Therapeutics Inc.
Flare Therapeutics is a clinical-stage biotechnology company exclusively focused on drugging transcription factors to fully unlock the therapeutic potential of this previously elusive target class. The company’s lead program, FX-909, is a first-in-class orally available small molecule inhibitor of PPARG, a master regulator of the luminal lineage, that is initially being developed for locally advanced or metastatic urothelial cancer. FX-909 has achieved clinical proof-of-concept in a Phase 1A study as a monotherapy and is actively dosing patients in a Phase 1B to determine the recommended Phase 2 dose in a biomarker-defined population. The second lead program, FX-111, is a novel and highly differentiated potent and selective degrader for ARON, the transcriptionally active, hormone-bound androgen receptor. This approach offers the potential to overcome key vulnerabilities of conventional therapies that target AROFF and has broad potential across prostate cancer at all stages. FX-111 is undergoing Investigational New Drug (IND)-enabling studies for initial development for the treatment of metastatic castration-resistant prostate cancer (mCRPC). These two programs, along with an earlier-stage portfolio targeting transcription factors involved in oncology and other therapeutic areas, leverages Flare Therapeutics’ integrated discovery platform of capabilities that identifies novel validated ligands to the undrugged proteome. For more information, please visit www.flaretx.com and follow us on LinkedIn.
Contacts:
Investors:
Sarah McCabe
investorrelations@flaretx.com
Media:
media@flaretx.com
Clinical proof-of-concept achieved in Phase 1A study for FX-909, a first-in-class orally available small molecule inhibitor of PPARG
Cambridge, MA, August 5, 2025 — Flare Therapeutics Inc. (FlareTx), a clinical-stage biotechnology company targeting transcription factors to discover precision medicines for oncology and other therapeutic areas, today announced that it has dosed the first patients in its Phase 1B clinical trial evaluating FX-909, a first-in-class orally available small molecule inhibitor of PPARG, a master regulator of the luminal lineage, for the treatment of locally-advanced or metastatic urothelial cancer (UC). More information about the trial is available at clinicaltrials.gov using the identifier NCT05929235.
“The initiation of the Phase 1B expansion study marks an important milestone as we seek to improve the treatment of advanced urothelial cancer with our lead program FX-909,” said Doug Manion, M.D., FRCP (C), Chief Executive Officer and Board Member. “We are prospectively screening for patients with high expression of PPARG, the hallmark of the luminal lineage, which accounts for approximately 65% of cases of advanced UC. We believe our PPARG inhibitor approach in this defined patient population represents a significant step toward addressing the disease at its source. By introducing a novel nuclear hormone receptor therapy—akin to the critical roles AR and ER play in prostate and breast cancers, respectively—we are expanding the therapeutic landscape to directly target the cell of origin and address the underlying disease biology.”
FX-909 has achieved clinical proof-of-concept in a Phase 1A study, as a monotherapy, based on pre-specified criteria. The company expects to present these data at a scientific conference in 2025. The Phase 1B study will evaluate safety and efficacy to determine the recommended Phase 2 dose in a biomarker-defined population. A validated immunohistochemistry (IHC)-based test is being deployed to prospectively select patients with the lineage determining transcription factor that drives the initiation and progression of these tumor types. The study will evaluate 30 mg and 50 mg (QD) doses in a 2-stage design, enrolling approximately 40 patients in total.
The company expects to report efficacy data in a biomarker-defined population at the recommended Phase 2 dose in the first quarter of 2026.
About Advanced Urothelial Cancer
Advanced urothelial cancer (UC) is an aggressive and challenging form of bladder cancer, representing approximately 25% of all bladder cancers diagnosed each year. In the United States, bladder cancer accounts for approximately 84,000 new cases each year, with urothelial carcinoma being the predominant histologic type. In advanced or metastatic stages, the disease is notably difficult to treat, with over 50% of patients experiencing disease progression within six to nine months of first-line chemotherapy. The five-year survival rate for metastatic UC remains poor, with estimates below 6%. While the introduction of checkpoint inhibitors and targeted therapies has expanded treatment options, clinical outcomes remain suboptimal, underscoring an urgent need for additional and more effective treatment options. Molecular subtyping has revealed that luminal tumors, or tumors that are characterized by high PPARG expression, comprise approximately 65% of advanced urothelial cancers. These luminal tumors are often or invariably characterized by activation of the PPARG (peroxisome proliferator-activated receptor gamma) pathway, which plays a critical role in maintaining tumor identity, promoting tumor growth, and contributing to immune evasion. Novel approaches such as PPARG inhibition are emerging as promising strategies to improve outcomes for patients that have UC with high PPARG expression. It is estimated that the United States alone, there are approximately 14,000 new cases of advanced urothelial cancer with high PPARG expression diagnosed each year, based on the portion of luminal subtypes and overall incidence data.
About Flare Therapeutics Inc.
Flare Therapeutics is a clinical-stage biotechnology company exclusively focused on drugging transcription factors to fully unlock the therapeutic potential of this previously elusive target class. The company’s lead program, FX-909, is a first-in-class orally available small molecule inhibitor of PPARG, a master regulator of the luminal lineage, that is initially being developed for locally advanced or metastatic urothelial cancer. FX-909 has achieved clinical proof-of-concept in a Phase 1A study as a monotherapy and is actively dosing patients in a Phase 1B to determine the recommended Phase 2 dose in a biomarker-defined population. The second lead program, FX-111, is a novel and highly differentiated potent and selective degrader for ARON, the transcriptionally active, hormone-bound androgen receptor. This approach offers the potential to overcome key vulnerabilities of conventional therapies that target AROFF and has broad potential across prostate cancer at all stages. FX-111 is undergoing Investigational New Drug (IND)-enabling studies for initial development for the treatment of metastatic castration-resistant prostate cancer (mCRPC). These two programs, along with an earlier-stage portfolio targeting transcription factors involved in oncology and other therapeutic areas, leverages Flare Therapeutics’ integrated discovery platform of capabilities that identifies novel validated ligands to the undrugged proteome. For more information, please visit www.flaretx.com and follow us on LinkedIn.
Contacts:
Investors:
Sarah McCabe
Media:
Cambridge, MA, May 28, 2025 — Flare Therapeutics Inc. (FlareTx), a clinical-stage biotechnology company targeting transcription factors to discover precision medicines for oncology and other therapeutic areas, today announced that the company will participate in meetings with investors at the upcoming Jefferies Global Healthcare Conference on Tuesday, June 3, 2025, in New York, NY.
About Flare Therapeutics Inc.
Flare Therapeutics is a clinical-stage biotechnology company exclusively focused on drugging transcription factors to fully unlock the therapeutic potential of this previously elusive target class. The company’s lead program, FX-909, is a first-in-class orally available small molecule inhibitor of PPARG, a master regulator of the luminal lineage, that is initially being developed for locally-advanced or metastatic urothelial cancer. FX-909 has achieved clinical proof-of-concept in a Phase 1A study as a monotherapy, and is progressing into Phase 1B to determine the recommended Phase 2 dose in a biomarker-defined population, and will include a combination arm with an anti-PD1-targeting agent. The second lead program, FX-111, is a novel and highly differentiated potent and selective degrader for ARON, the transcriptionally active, hormone-bound conformation of the androgen receptor. This approach offers the potential to overcome key vulnerabilities of conventional therapies that target AROFF and has broad potential across prostate cancer at all stages. FX-111 is undergoing Investigational New Drug (IND)-enabling studies for initial development for the treatment of metastatic castration-resistant prostate cancer (mCRPC). These two programs, along with an earlier-stage portfolio targeting transcription factors involved in oncology and other therapeutic areas, leverages Flare Therapeutics’ integrated discovery platform of capabilities that identifies novel validated ligands to the undrugged proteome. For more information, please visit www.flaretx.com and follow us on LinkedIn.
Contacts:
Investors:
Media:
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