GPR119

Full Data Readout Expected in the Second Half of 2024 CAMBRIDGE, Mass., Jan. 18, 2024 /PRNewswire/ -- NeuroBo Pharmaceuticals, Inc. (Nasdaq: NRBO), a clinical-stage biotechnology company focused on transforming cardiometabolic diseases, today announced positive pre-clinical safety data of DA-1241, a novel G-Protein-Coupled Receptor 119 (GPR119) agonist, in combination with sitagliptin, a DPP4 inhibitor. Additionally, having satisfied its 45-day commitment with the U.S. Food and Drug Administration (FDA) related to its amended protocol, the company has opened enrollment for Part 2 of its Phase 2a clinical trial of DA-1241 when co-administered with sitagliptin for the treatment of metabolic dysfunction-associated steatohepatitis (MASH). The pre-clinical results demonstrated that once daily oral administration in rats, of sitagliptin alone (180 mg/kg/day), DA-1241 alone (100 mg/kg/day), or sitagliptin in combination with DA-1241 (up to 180/100 mg/kg/day sitagliptin+DA-1241) for 13 weeks, was well tolerated with no adverse effects. "Initiating Part 2 of our clinical study of DA-1241 in MASH patients paves the way to begin dosing in combination with sitagliptin, marking another significant clinical milestone for our most advanced asset," stated Hyung Heon Kim, President and Chief Executive Officer of NeuroBo. "Based on the pre-clinical evidence to date, DA-1241 has been shown to improve both hepatic and systemic inflammation effectively, and the combination with sitagliptin increased the anti-inflammatory effects compared to DA-1241 as a monotherapy. As previously reported, DA-1241 was also well tolerated in healthy volunteers and in patients with type 2 diabetes mellitus (T2DM). Given the totality of this data, we believe that the mechanism of action could allow DA-1241 to become a safe and effective treatment for MASH, and its anti-MASH and anti-diabetic effects could be potentiated when co-administered with a DPP4 inhibitor. We expect to report the full data from the Part 2 trial in the second half of 2024." Each of the two-parts of the Phase 2a trial of DA-1241 is designed to be a 16-week, multicenter, randomized, double-blind, placebo-controlled, parallel clinical study to evaluate the efficacy and safety of DA-1241 in subjects with presumed MASH. Part 1, currently dosing subjects, is exploring the efficacy of DA-1241 versus placebo, and is expected to enroll approximately 49 subjects, who will be randomized in a 1:2:1 ratio into 3 treatment groups: DA-1241 50 mg, DA-1241 100 mg, or placebo. Part 2 will explore the efficacy of DA-1241 in combination with sitagliptin, versus placebo, is expected to enroll approximately 37 subjects, who will be randomized in a 2:1 ratio into 2 treatment groups: DA-1241 100 mg/sitagliptin 100 mg or placebo. For both Part 1 and Part 2, the primary endpoint is the change from baseline in alanine transaminase (ALT) levels at Week 16. Secondary efficacy endpoints include the proportion of subjects with normalization of ALT, absolute change in total cholesterol, low and high-density lipoprotein cholesterol, triglyceride, and free fatty acids from baseline, among others. Safety will be evaluated by monitoring adverse events (AEs), serious adverse events (SAEs) and AEs leading to discontinuation and laboratory abnormalities. About DA-1241 DA-1241 is a novel G-Protein-Coupled Receptor 119 (GPR119) agonist with development optionality as a standalone and/or combination therapy for both MASH and T2DM. In preclinical studies, DA-1241 demonstrated that GPR-119 agonism promotes the release of the key gut peptides GLP-1, GIP, and PYY, which have a beneficial effect on liver inflammation, lipid metabolism, weight loss, and glucose metabolism. The therapeutic potential of DA-1241 has been demonstrated in multiple pre-clinical animal models of MASH and T2DM whereby DA-1241 reduced hepatic steatosis, hepatic inflammation, and liver fibrosis, while also improving glucose control. Furthermore, in Phase 1a and 1b trials, DA-1241 was well tolerated in both healthy volunteers and those with T2DM. About NeuroBo Pharmaceuticals NeuroBo Pharmaceuticals, Inc. is a clinical-stage biotechnology company focused on transforming cardiometabolic diseases. The company is currently developing DA-1241 for the treatment of Metabolic Dysfunction-Associated Steatohepatitis (MASH) and Type 2 Diabetes Mellitus (T2DM), and is developing DA-1726 for the treatment of obesity. DA-1241 is a novel G-protein-coupled receptor 119 (GPR119) agonist that promotes the release of key gut peptides GLP-1, GIP, and PYY. In preclinical studies, DA-1241 demonstrated a positive effect on liver inflammation, lipid metabolism, weight loss, and glucose metabolism, reducing hepatic steatosis, hepatic inflammation, and liver fibrosis, while also improving glucose control. DA-1726 is a novel oxyntomodulin (OXM) analogue that functions as a glucagon-like peptide-1 receptor (GLP1R) and glucagon receptor (GCGR) dual agonist. OXM is a naturally-occurring gut hormone that activates GLP1R and GCGR, thereby decreasing food intake while increasing energy expenditure, thus potentially resulting in superior body weight loss compared to selective GLP1R agonists. For more information, please visit . Forward Looking Statements Certain statements in this release may be considered forward-looking statements within the meaning of the Private Securities Litigation Reform Act of 1995. Words such as "believes", "expects", "anticipates", "may", "will", "should", "seeks", "approximately", "intends", "projects," "plans", "estimates" or the negative of these words or other comparable terminology (as well as other words or expressions referencing future events, conditions or circumstances) are intended to identify forward-looking statements. Forward-looking statements are predictions, projections and other statements about future events that are based on current expectations and assumptions and, as a result, are subject to risks and uncertainties. Many factors could cause actual future events to differ materially from the forward-looking statements in this release, including, without limitation, those risks associated with NeuroBo's ability to execute on its commercial strategy; the timeline for regulatory submissions; ability to obtain regulatory approval through the development steps of NeuroBo's current and future product candidates, the ability to realize the benefits of the license agreement with Dong-A ST Co. Ltd., including the impact on future financial and operating results of NeuroBo; the cooperation of our contract manufacturers, clinical study partners and others involved in the development of NeuroBo's current and future product candidates; potential negative interactions between our product candidates and any other products with which they are combined for treatment; NeuroBo's ability to initiate and complete clinical trials on a timely basis; our ability to recruit subjects for its clinical trials; whether NeuroBo receives results from NeuroBo's clinical trials that are consistent with the results of pre-clinical and previous clinical trials; impact of costs related to the license agreement, known and unknown, including costs of any litigation or regulatory actions relating to the license agreement; effects of changes in applicable laws or regulations; effects of changes to NeuroBo's stock price on the terms of the license agreement and any future fundraising; and other risks and uncertainties described in our filings with the SEC. Forward-looking statements speak only as of the date when made. NeuroBo does not assume any obligation to publicly update or revise any forward-looking statements, whether as a result of new information, future events or otherwise, except as required by law. Contacts: NeuroBo Pharmaceuticals Marshall H. Woodworth Interim Chief Financial Officer +1-857-299-1033 [email protected] Rx Communications Group Michael Miller +1-917-633-6086 [email protected] SOURCE NeuroBo Pharmaceuticals, Inc.

Two-Part Design Provides Optionality for Interim Analysis in First Half of 2024 Full Data Readout Expected in the Second Half of 2024 BOSTON, Sept. 15, 2023 /PRNewswire/ -- NeuroBo Pharmaceuticals, Inc. (Nasdaq: NRBO), a clinical-stage biotechnology company on a quest to transform cardiometabolic diseases, today announced dosing of the first patient in its two-part, Phase 2a clinical trial of DA-1241, a novel G-Protein-Coupled Receptor 119 (GPR119) agonist, for the treatment of nonalcoholic steatohepatitis (NASH), at The Pinnacle Edinberg/South Texas Research Institute in Edinburg, Texas, under the supervision of Principal Investigator, Dr. David Ramirez. "Dosing the first patient, on time, is a testament to our commitment to the clinical development of DA-1241 in patients with NASH," stated Hyung Heon Kim, President and Chief Executive Officer of NeuroBo. "Based on the pre-clinical and clinical evidence generated to date, DA-1241 has demonstrated reduced hepatic steatosis, hepatic inflammation, and liver fibrosis, while also improving glucose control, and was shown to be well tolerated in both healthy volunteers and in patients with type 2 diabetes mellitus (T2DM). Given this data, we believe that the mechanism of action of this promising cardiometabolic asset will translate into a safe and effective treatment for NASH, a disease with no current treatment options. The two-part design of this trial provides optionality for a potential interim analysis in the first half of 2024 and we expect to report the full data in the second half of 2024." Each of the two-parts of the Phase 2a trial of DA-1241 is designed to be a 16-week, multicenter, randomized, double-blind, placebo-controlled, parallel clinical study to evaluate the efficacy and safety of DA-1241 in subjects with presumed NASH and confirmed pre-diabetes or T2DM. Part 1 will explore the efficacy of DA-1241 versus placebo, and is expected to enroll 49 subjects, with a planned maximum of 55 subjects to account for early discontinuations. Subjects will be randomized in a 1:2:1 ratio into 3 treatment groups: DA-1241 50 mg, DA-1241 100 mg, or placebo. Part 2 will explore the efficacy of DA-1241 in combination with sitagliptin, versus placebo, and will begin after completion of a confirmatory preclinical safety study of DA-1241 in combination with sitagliptin. It is expected to enroll 37 subjects, with a planned maximum of 43 subjects to account for early discontinuations, and subjects will be randomized in 2:1 ratio into 2 treatment groups: DA-1241 100 mg/sitagliptin 100 mg or placebo. For both Part 1 and Part 2, the primary endpoint is the change from baseline in alanine transaminase (ALT) levels at Week 16. Secondary efficacy endpoints include the proportion of subjects with normalization of ALT, absolute change in total cholesterol, low and high-density lipoprotein cholesterol, triglyceride, and free fatty acids from baseline, among others. Safety will be evaluated by monitoring adverse events (AEs), serious adverse events (SAEs) and AEs leading to discontinuation and laboratory abnormalities. About DA-1241 DA-1241 is a novel G-Protein-Coupled Receptor 119 (GPR119) agonist with development optionality as a standalone and/or combination therapy for both NASH and T2DM. In preclinical studies, DA-1241 demonstrated that GPR-119 agonism promotes the release of the key gut peptides GLP-1, GIP, and PYY, which have a beneficial effect on liver inflammation, lipid metabolism, weight loss, and glucose metabolism. The therapeutic potential of DA-1241 has been demonstrated in multiple pre-clinical animal models of NASH and T2DM whereby DA-1241 reduced hepatic steatosis, hepatic inflammation, and liver fibrosis, while also improving glucose control. Furthermore, in Phase 1a and 1b trials, DA-1241 was well tolerated in both healthy volunteers and those with T2DM. About NeuroBo Pharmaceuticals NeuroBo Pharmaceuticals, Inc. is a clinical-stage biotechnology company on a quest to transform cardiometabolic diseases. The company is currently developing DA-1241 for the treatment of Non-Alcoholic Steatohepatitis (NASH) and Type 2 Diabetes Mellitus (T2DM), and is developing DA-1726 for the treatment of obesity. DA-1241 is a novel G-Protein-Coupled Receptor 119 (GPR119) agonist, which promotes the release of key gut peptides GLP-1, GIP, and PYY. In preclinical studies, DA-1241 demonstrated positive effect on liver inflammation, lipid metabolism, weight loss, and glucose metabolism, reducing hepatic steatosis, hepatic inflammation, and liver fibrosis, while also improving glucose control. DA-1726 is a novel oxyntomodulin (OXM) analogue that acts as a glucagon-like peptide-1 receptor (GLP1R) and glucagon receptor (GCGR) dual agonist. OXM is a naturally-occurring gut hormone that activates GLP1R and GCGR, thereby decreasing food intake while increasing energy expenditure, thus potentially resulting in superior body weight loss compared to selective GLP1R agonists. For more information, please visit . Forward Looking Statements Certain statements in this release may be considered forward-looking statements within the meaning of the Private Securities Litigation Reform Act of 1995, including without limitation, statements about the closing of the offering of securities. Forward-looking statements are predictions, projections and other statements about future events that are based on current expectations and assumptions and, as a result, are subject to risks and uncertainties. Many factors could cause actual future events to differ materially from the forward-looking statements in this release, including, without limitation, those risks associated with our ability to execute on our commercial strategy, the timeline for regulatory submissions, regulatory steps and potential regulatory approval of our current and future product candidates, the ability to realize the benefits of the license agreement with Dong-A ST Co. Ltd., including the impact on future financial and operating results of NeuroBo; the ability to integrate the new product candidates into NeuroBo's business in a timely and cost-efficient manner; the cooperation of our contract manufacturers, clinical study partners and others involved in the development of our current and future product candidates; our ability to initiate and complete clinical trials on a timely basis; our ability to recruit subjects for our clinical trials; receiving results from our clinical trials that are consistent with the results of pre-clinical and previous clinical trials; costs related to the license agreement, known and unknown, including costs of any litigation or regulatory actions relating to the license agreement; changes in applicable laws or regulations; effects of changes to NeuroBo's stock price on the terms of the license agreement and any future fundraising; and other risks and uncertainties described in our filings with the SEC. Forward-looking statements speak only as of the date when made. NeuroBo does not assume any obligation to publicly update or revise any forward-looking statements, whether as a result of new information, future events or otherwise. Contact: Rx Communications Group Michael Miller +1-917-633-6086 [email protected] SOURCE NeuroBo Pharmaceuticals, Inc.

13-Week Study to Evaluate the Safety and Efficacy of VK2735 Dosed Weekly SAN DIEGO, CA, USA I September 6, 2023 I Viking Therapeutics, Inc. (Viking) (NASDAQ: VKTX ), a clinical-stage biopharmaceutical company focused on the development of novel therapies for metabolic and endocrine disorders, today announced the initiation of a Phase 2 clinical trial of VK2735, the company's wholly-owned dual agonist of the glucagon-like peptide 1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP) receptors.  VK2735 is in development for the potential treatment of various metabolic disorders such as obesity. The Phase 2 VENTURE trial is a randomized, double-blind, placebo-controlled study that will evaluate the safety, tolerability, pharmacokinetics, and weight loss efficacy of four different doses of VK2735, administered subcutaneously, once weekly.  The 13-week trial will enroll approximately 125 adults who are obese (BMI ≥30 kg/m 2 ), or adults who are overweight (BMI ≥27 kg/m 2 ) with at least one weight-related co-morbid condition.  The primary endpoint of the study is the percent change in body weight from baseline to Week 13, with secondary and exploratory endpoints evaluating a range of additional safety and efficacy measures. "We are excited to announce the initiation of the VENTURE study, which will build upon the promising VK2735 Phase 1 data we reported earlier this year," said Brian Lian, Ph.D., chief executive officer of Viking. "Obesity is a major healthcare challenge, and recent data confirm that effective weight loss agents can reduce a patient's cardiovascular risk profile, providing important health benefits.  We look forward to exploring VK2735's safety and weight loss efficacy over this study's 13-week dosing window." Viking previously reported positive results from a Phase 1 single ascending dose (SAD) and multiple ascending dose (MAD) clinical trial of VK2735 in healthy volunteers with a BMI ≥30.  In the SAD portion of the study, VK2735 demonstrated promising safety and tolerability, as well as a predictable pharmacokinetic profile.  In the 28-day MAD portion of the study, VK2735 was well-tolerated and showed positive signs of clinical activity.  All MAD cohorts receiving VK2735 experienced reductions in mean body weight from baseline, ranging up to 7.8%.  Cohorts receiving VK2735 also demonstrated reductions in mean body weight relative to placebo, ranging up to 6.0%.  Statistically significant differences compared to placebo were maintained or improved at the Day 43 follow-up time point, 21 days after the last dose of VK2735 was administered. The majority of observed adverse events (98%) in the Phase 1 trial were reported as mild or moderate.  The majority of GI-specific adverse events (99%) were also reported as mild or moderate.  Notably, despite robust activation of the incretin receptor pathways, no hypoglycemia was reported.  The company believes that the tolerability data from the Phase 1 study indicate that higher doses may be achieved with longer titration windows. Viking is also conducting a Phase 1 trial of a novel oral formulation of VK2735, which it believes may significantly expand the market opportunity for the compound by offering patients the option between subcutaneous and oral dosages forms.  The company expects to report initial data from the oral formulation Phase 1 study in the fourth quarter of 2023. About GLP-1 and Dual GLP-1/GIP Agonists Activation of the glucagon-like peptide 1 (GLP-1) receptor has been shown to decrease glucose, reduce appetite, lower body weight, and improve insulin sensitivity in patients with type 2 diabetes, obesity, or both. Semaglutide is a GLP-1 receptor agonist that has been approved by the U.S. Food and Drug Administration and is currently marketed in various dosage strengths and forms as Ozempic ® , Rybelsus ® , and Wegovy ® . More recently, research efforts have explored the potential co-activation of the glucose-dependent insulinotropic peptide (GIP) receptor as a means of enhancing the therapeutic benefits of GLP-1 receptor activation. Tirzepatide is a dual GLP-1/GIP receptor agonist that is currently in clinical development for obesity. About Viking Therapeutics, Inc. Viking Therapeutics is a clinical-stage biopharmaceutical company focused on the development of novel first-in-class or best-in-class therapies for the treatment of metabolic and endocrine disorders, with three compounds currently in clinical trials. Viking's research and development activities leverage its expertise in metabolism to develop innovative therapeutics designed to improve patients' lives. The company's clinical programs include VK2809, a novel, orally available, small molecule selective thyroid hormone receptor beta agonist for the treatment of lipid and metabolic disorders, which is currently being evaluated in a Phase 2b study for the treatment of biopsy-confirmed non-alcoholic steatohepatitis (NASH) and fibrosis. In a Phase 2a trial for the treatment of non-alcoholic fatty liver disease (NAFLD) and elevated LDL-C, patients who received VK2809 demonstrated statistically significant reductions in LDL-C and liver fat content compared with patients who received placebo. The company is also developing VK2735, a novel dual agonist of the glucagon-like peptide 1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP) receptors for the potential treatment of various metabolic disorders. Data from a Phase 1 trial evaluating VK2735 (dosed subcutaneously) for metabolic disorders demonstrated an encouraging safety and tolerability profile as well as positive signs of clinical benefit. The company also recently initiated a Phase 1 study to evaluate an oral formulation of VK2735. In the rare disease space, the company is developing VK0214, a novel, orally available, small molecule selective thyroid hormone receptor beta agonist for the potential treatment of X-linked adrenoleukodystrophy (X-ALD). VK0214 is currently being evaluated in a Phase 1b clinical trial in patients with the adrenomyeloneuropathy (AMN) form of X-ALD. The company holds exclusive worldwide rights to a portfolio of five therapeutic programs, including VK2809 and VK0214, which are based on small molecules licensed from Ligand Pharmaceuticals Incorporated. For more information about Viking Therapeutics, please visit www.vikingtherapeutics.com . Follow Viking on Twitter @Viking_VKTX. SOURCE: Viking Therapeutics