Delving into the Latest Updates on Efinopegdutide with Synapse

Overview

Basic Info

Drug Type

Synthetic peptide

Synonyms

Efinopegdutide (USAN/INN), GLP-1/glucagon-agonist, Glucagon-like-peptides/glucagon

+ [13]

Target

GCGR x GLP-1R

Mechanism

GCGR agonists(Glucagon receptor agonists), GLP-1R agonists(Glucagon-like peptide 1 receptor agonists)

Therapeutic Areas

Digestive System DisordersEndocrinology and Metabolic Disease

Active Indication

Liver CirrhosisNonalcoholic fatty liverNonalcoholic Steatohepatitis+ [2]

Inactive Indication

Diabetes Mellitus, Type 2Kidney Failure, ChronicType 2 diabetes mellitus in obese

Originator Organization

Hanmi Pharmaceutical Co., Ltd.

Active Organization

MSD R&D (China) Co. Ltd.

Merck Sharp & Dohme Corp.Merck Sharp & Dohme LLC

+ [1]

Inactive Organization

Janssen Research & Development LLC

Janssen Pharmaceuticals, Inc.

Drug Highest PhasePhase 2

First Approval Date-

RegulationFast Track (US)

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Gene Sequence

Sequence Code 9133009

Source: *****

Sequence Code 1191632819

Source: *****

Researchers are looking for ways to treat a type of liver disease caused by elevated liver fat, called metabolic dysfunction-associated steatohepatitis (MASH). MASH was formerly called non-alcoholic steatohepatitis (NASH). Researchers want to learn if a study medicine called efinopegdutide can treat MASH.The goals of this study are to learn:
* If efinopegdutide can lower the amount of fat, inflammation, and scarring (fibrosis) in the liver
* About the safety of efinopegdutide and how well people tolerate it

Start Date12 Jul 2024

Sponsor / Collaborator

Merck Sharp & Dohme LLC

100 Clinical Results associated with Efinopegdutide

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100 Translational Medicine associated with Efinopegdutide

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100 Patents (Medical) associated with Efinopegdutide

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224

Literatures (Medical) associated with Efinopegdutide

01 Nov 2024·EUROPEAN JOURNAL OF PHARMACEUTICAL SCIENCES

Absorption, distribution, metabolism, and excretion of tirzepatide in humans, rats, and monkeys

Article

Author: Cassidy, Kenneth C ; Czeskis, Boris ; Martin, Jennifer A ; Urva, Shweta

Tirzepatide is a once-weekly GIP/GLP-1 receptor agonist used for treatment of type 2 diabetes (T2D) in adults and was recently approved for treatment of obesity. To determine the absorption, distribution, metabolism, and excretion (ADME) of tirzepatide, [¹⁴C]-radiolabeled tirzepatide was investigated in both humans and preclinical species. [¹⁴C]-Tirzepatide was prepared by incorporating four ¹⁴C's in the linker region between the amino acid backbone and the di-acid moiety. Healthy male participants received a single subcutaneous dose of approximately 2.9 mg tirzepatide containing approximately 100 μCi of [¹⁴C]-tirzepatide. Preclinical studies were conducted in male Sprague Dawley and Long Evans rats administered a single dose of 3 mg kg^-1 (133 µCi/kg) of [¹⁴C]-tirzepatide, and male cynomolgus monkeys administered a single dose of 0.5 mg kg^-1 (20 µCi/kg) of [¹⁴C]-tirzepatide. Following a single SC dose of [¹⁴C]-tirzepatide in humans, the majority of the excreted dose was recovered within 480 h. Renal excretion was identified as a principal route of elimination in all species with approximately 66 % of the administered radioactivity recovered in urine, while approximately 33 % was eliminated in feces in humans. Metabolite analysis of tirzepatide revealed the parent drug was the major circulating component in human, rat, and monkey plasma. Metabolites identified in human plasma were similar to circulating metabolites found in rats and monkeys with no circulating metabolites representing >10 % of the total radioactive drug-related exposure. Intact tirzepatide was not observed in urine or feces in any species. Tirzepatide was primarily metabolized via proteolytic cleavage of the amino acid backbone, β-oxidation of the C20 diacid moiety, and amide hydrolysis. ClinicalTrials.gov identifier: NCT 04,311,424.

01 Oct 2024·ANALYTICAL BIOCHEMISTRY

Implementation of a LC-MS based multi-attribute method (MAM) and intact multi-attribute method (iMAM) workflow for the characterisation of a GLP-Fc fusion protein

Article

Author: Bones, Jonathan ; MacHale, Ciara ; Buckley, Ciarán ; Millán-Martín, Silvia ; Füssl, Florian ; Carillo, Sara

Over the past few years, the implementation of mass spectrometry (MS) in QC laboratories has become a more common occurrence. The multi-attribute method (MAM), and emerging intact multi-attribute method (iMAM), are powerful analytical tools utilising liquid chromatography-mass spectrometry (LC-MS) methods that enable the monitoring of critical quality attributes (CQAs) in biotherapeutic proteins in compliant settings. Both MAM and iMAM are intended to replace or supplement several conventional assays with a single LC-MS method utilising MS data in combination with robust, semi-automated data processing workflows. MAM and iMAM workflows can also be implemented into current Good Manufacturing Practices environments due to the availability of CFR 11 compliant chromatography data system software. In this study, MAM and iMAM are employed for the analysis of 4 batches of a glucagon-like peptide-Fc fusion protein. MAM approach involved a first the discovery phase for the identification of CQAs and second, the target monitoring phase of the selected CQAs in other samples. New peak detection was performed on the data set to determine the appearance, absence or change of any peak. For native iMAM workflow both size exclusion and strong cation exchange chromatography were optimized for the identification and monitoring of CQAs at the intact level.

02 Aug 2024·Expert Review of Clinical Pharmacology

Lipid profile changes induced by glucagon-like peptide-1 receptor agonists in patients with type 2 diabetes: a systematic review and network meta-analysis

Review

Author: Kim, Hyo-Jin ; Chae, Yuna ; Kwon, Sun-Hong ; Kang, Eunsung ; Nam, Jin Hyun ; Lee, Eui-Kyung ; Im, Jiae

OBJECTIVE:

This study was conducted to investigate the effects of glucagon-like peptide-1 receptor (GLP-1) agonists on the lipid profiles of patients with type 2 diabetes.

METHODS:

We retrieved the data of phase 3 randomized controlled trials on GLP-1 agonists in patients with type 2 diabetes from the PubMed, Embase, and Cochrane library up to 11 February 2024. We extracted % changes in low-density lipoprotein cholesterol (LDL-C)/high-density lipoprotein cholesterol/total cholesterol (T-CHO) and triglycerides levels from baseline. Using Bayesian network meta-analysis, mean differences and 95% credible intervals for lipid changes were estimated as a unit of percentage points (%p) by class.

RESULTS:

Twenty-six studies covering 22,290 participants were included. The glucose-dependent insulinotropic polypeptide (GIP)/GLP-1 dual agonist showed significant differences in LDL-C (range of mean differences: -11.61 to -6.77%p), triglycerides (-19.94 to -13.31%p), and T-CHO (-7.94 to -5.09%p) levels compared to placebo, insulin, and sodium-glucose co-transporter 2 (SGLT2) inhibitors. The GLP-1 agonist significantly reduced T-CHO (-5.20%p; -6.39%p) and LDL-C (-4.32%p; -8.17%p) levels compared to placebo and SGLT2 inhibitors, respectively.

CONCLUSIONS:

The GIP/GLP-1 dual agonist positively affects the lipid profiles of patients with type 2 diabetes. This may contribute to a lower risk of cardiovascular disease in patients with type 2 diabetes.

PROTOCOL REGISTRATION:

PROSPERO (CRD42021282668).

196

News (Medical) associated with Efinopegdutide

22 Oct 2024

·www.pharmaceutical-technology.com

Novo Nordisk plans label expansion for Rybelsus following Phase III win

Novo Nordisk’s Rybelsus is an oral semaglutide, approved for treating type 2 diabetes. Image credit: JHVEPhoto / Shutterstock. Novo Nordisk plans to file a label expansion for Rybelsus (oral semaglutide) as an adjunct treatment for the prevention of major adverse cardiovascular events (MACE) in patients with type 2 diabetes (T2D) and established cardiovascular disease (CVD) and/or chronic kidney disease (CKD). The Phase III SOUL trial (NCT03914326) met its primary endpoint by reducing the occurrence of MACE by 14% with Rybelsus compared to placebo. The study defined the composite outcome of the first occurrence of MACE as cardiovascular death, non-fatal myocardial infarction, or non-fatal stroke. Novo Nordisk intends to file for regulatory approval for Rybelsus label expansion in the indication in the US and Europe in late 2024/early 2025. The US Food and Drug Administration (FDA) approved the once-daily pill as a treatment for T2D in 2019. If approved, Rybelsus will be the second semaglutide medication by Novo Nordisk authorised in the cardiovascular setting. In March, the FDA approved an injectable formulation of semaglutide, Wegovy , for the reduction in the risk of cardiovascular death, heart attack, and stroke in adults with heart disease who are diagnosed as obese or overweight. The diabetes and obesity segment generated DKr215bn ($31.2bn) in sales for Novo Nordisk, as per the company’s financials. Rybelsus contributed DKr18.7bn ($2.1bn) in sales last year and GlobalData expects the therapy’s sales to exceed $6.8bn in 2030. See Also: Gilead and MSD to advance once-weekly HIV treatment to Phase III Editas and Genevant team up to develop gene editing therapies GlobalData is the parent company of Pharmaceutical Technology . The Phase III SOUL trial enrolled 9,650 patients with T2D and established CVD and/or CKD. The participants received either Rybelsus or a placebo in addition to the standard of care, including sodium-glucose cotransporter-2 inhibitors (SGLT2i) with which 49% of the participants were treated. Novo Nordisk plans to present full detailed results from the trial at a scientific conference next year. Novo Nordisk’s competitor Eli Lilly is also looking to expand the label for its diabetes and obesity therapies. In August, Lilly presented data showing that its triple GLP-1/GIP/glucagon receptor agonist, retatrutide, improved cardiac outlook and reduced serum lipids in obese or overweight patients.

Phase 3Drug ApprovalClinical Result

01 Oct 2024

·www.fiercebiotech.com

Kailera launches with $400M series A and clutch of Chinese obesity drugs

Kailera Therapeutics' funding was co-led by Atlas Venture, Bain Capital Life Sciences and RTW Investments. Kailera Therapeutics has launched into the increasingly crowded obesity space with a portfolio of assets acquired from China and $400 million in series A funds.The Massachusetts- and California-based biotech is led by former Cerevel Therapeutics CEO Ron Renaud. Kailera may only be stepping into the spotlight today, but it secured the ex-China rights to four GLP-1 drugs from Jiangsu Hengrui Pharmaceuticals back in May.Top of the pile is HRS9531, now rebranded as KAI-9531, an injectable GLP-1/GIP receptor dual agonist that Kailera said has already demonstrated “compelling results” in phase 2 trials for obesity and Type 2 diabetes in China. There is also another clinical-stage asset in the form of an oral small molecule GLP-1 receptor agonist, followed by a once-daily oral GLP-1/GIP receptor dual agonist and an injectable GLP-1/GIP/glucagon receptor tri-agonist.Kailera will be joining an ever-growing list of Big Pharmas and small biotechs hoping that some combination of GLP-1 and GIP agonists can carve out space in an obesity market currently dominated by Novo Nordisk's Wegovy and Eli Lilly's Zepbound. But seasoned investors clearly see potential in the recently acquired assets. The $400 million series A was co-led by Atlas Venture, Bain Capital Life Sciences and RTW Investments, with participation from Lyra Capital.“In this period of rapid innovation in the metabolic space, I believe that Kailera is poised to make an impact beyond the current market leaders,” Kailera’s CEO Renaud said in a Oct. 1 release.“With a clinically-advanced, differentiated pipeline, a talented and experienced team with a track record for building companies with lasting impact, and the support of a world-class investor syndicate, we are uniquely positioned to advance innovative therapies that have the potential to meaningfully impact both quality of life and overall health for many people,” he added.Renaud oversaw neuroscience biotech Cerevel in the months leading up to its acquisition by AbbVie and has also served as a senior adviser at Bain Capital. He’s joining by Cereval alumni in the form of Kailera’s chief operating and chief business officer Paul Burgess, while former Latigo Biotherapeutics CEO Scott Wasserman, M.D., has been named chief medical officer.Meanwhile, former Gilead Sciences CEO John Milligan, Ph.D., is chairing Kailera’s board of directors.

Phase 2AcquisitionExecutive ChangePhase 1

01 Oct 2024

·www.prnewswire.com

NeuroBo Pharmaceuticals to Participate in Investor Conferences in October

CAMBRIDGE, Mass., Oct. 1, 2024 /PRNewswire/ -- NeuroBo Pharmaceuticals, Inc. (Nasdaq: NRBO), a clinical-stage biotechnology company focused on transforming cardiometabolic diseases, today announced that management will participate in the following investor conferences in October: October 7: H.C. Wainwright 8th Annual MASH Virtual Conference. Hyung Heon Kim, President and Chief Executive Officer, will present a company overview on Monday, October 7, at 11:00 am ET. Management will also be available for one-on-one meetings during the event. Individuals who would like to listen to the Company's presentation or request a meeting can do so after registering for the conference at . October 15-17: 2024 Maxim Healthcare Virtual Summit. Mr. Kim and Marshall H. Woodworth, Chief Financial Officer, will participate in a virtual fireside chat hosted by Jason McCarthy, Ph.D., senior managing director, head of biotechnology research at Maxim Group, on Tuesday, October 15, at 2:30 pm ET. To schedule a meeting with management outside of these conferences, investors can contact Michael Miller at [email protected]. About NeuroBo Pharmaceuticals NeuroBo Pharmaceuticals, Inc. is a clinical-stage biotechnology company focused on transforming cardiometabolic diseases. The company is currently developing DA-1726 for the treatment of obesity, and is developing DA-1241 for the treatment of Metabolic Dysfunction-Associated Steatohepatitis (MASH). 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. 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 pre-clinical 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. For more information, please visit . Contacts: NeuroBo Pharmaceuticals Marshall H. Woodworth Chief Financial Officer +1-857-299-1033 [email protected] Rx Communications Group Michael Miller +1-917-633-6086 [email protected] SOURCE NeuroBo Pharmaceuticals, Inc. WANT YOUR COMPANY'S NEWS FEATURED ON PRNEWSWIRE.COM? 440k+ Newsrooms & Influencers 9k+ Digital Media Outlets 270k+ Journalists Opted In GET STARTED

Phase 1

100 Deals associated with Efinopegdutide

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External Link

KEGG	Wiki	ATC	Drug Bank
D11607	-	-	DB15077

R&D Status

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Liver Cirrhosis	Phase 2	US	Merck Sharp & Dohme LLC	12 Jul 2024
Liver Cirrhosis	Phase 2	JP	Merck Sharp & Dohme LLC	12 Jul 2024
Liver Cirrhosis	Phase 2	AU	Merck Sharp & Dohme LLC	12 Jul 2024
Liver Cirrhosis	Phase 2	IL	Merck Sharp & Dohme LLC	12 Jul 2024
Liver Cirrhosis	Phase 2	PR	Merck Sharp & Dohme LLC	12 Jul 2024
Liver Cirrhosis	Phase 2	ES	Merck Sharp & Dohme LLC	12 Jul 2024
Liver Cirrhosis	Phase 2	GB	Merck Sharp & Dohme LLC	12 Jul 2024
Nonalcoholic fatty liver	Phase 2	US	Merck Sharp & Dohme Corp.	23 Jun 2023
Nonalcoholic fatty liver	Phase 2	CN	Merck Sharp & Dohme Corp.	23 Jun 2023
Nonalcoholic fatty liver	Phase 2	JP	Merck Sharp & Dohme Corp.	23 Jun 2023

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT04944992 (EudraCT: 2020-005136-30 \| MK-6024-001 \| 6024-001, CTgov)	Phase 2	Nonalcoholic Steatohepatitis	145	Efinopegdutide 20 mg/mL (Efinopegdutide)	dsahugxdwb(tvaqcjcfis) = lvrreaburz imsyrpfbax (hqdaqoakpg, kilkgxcggq - ystdjjaiue) View more	-	15 Nov 2023
				Semaglutide 1.34 mg/mL (Semaglutide)	dsahugxdwb(tvaqcjcfis) = sdkzlscwyf imsyrpfbax (hqdaqoakpg, yoefonpxkl - jcxdztoekn) View more
AASLD2023	Not Applicable	Metabolic dysfunction-associated steatotic liver disease	145	Efinopegdutide 10 mg QW	vgzeevfqnd(ygsnymkfkd) = wxqndhwyua onrtqxumjw (ziefxvkjis ) View more	-	10 Nov 2023
				Semaglutide 1.0 mg QW	vgzeevfqnd(ygsnymkfkd) = gdigxbsxio onrtqxumjw (ziefxvkjis ) View more
NCT04944992 (EudraCT: 2020-005136-30, EASD2023)	Phase 2	Diabetes Mellitus, Type 2 \| Metabolic dysfunction-associated steatotic liver disease	145	Efinopegdutide 10 mg	qeekmycntp(ktodevbndq) = dvxatexyym uqdwfeicas (leehvbybsz, 57.2 - 76.3) View more	Positive	04 Oct 2023
				Semaglutide 1 mg	qeekmycntp(ktodevbndq) = fmprgxfkzc uqdwfeicas (leehvbybsz, 36.0 - 55.1) View more
NCT04944992 (EudraCT: 2020-005136-30, Pubmed)	Phase 2	Metabolic dysfunction-associated steatotic liver disease	145	Efinopegdutide 10 mg	giqqprjicp(cfjpidygkp) = jemarotzvk xkcvhvtmbs (mvzbtzpfqy, 66.8 - 78.7) View more	Positive	01 Oct 2023
				Semaglutide 1 mg	giqqprjicp(cfjpidygkp) = lglhjbtcjp xkcvhvtmbs (mvzbtzpfqy, 36.5 - 48.1) View more
NCT03486392 (CTgov)	Phase 2	Obesity	474	placebo+JNJ-64565111 (Double Blind: Placebo)	gnukrwrnyf(bpuczuitrm) = zdneelxljp mkruuxgezc (chdqcyumuh, qvhuckgaay - brplnldusz) View more	-	05 Feb 2020
				JNJ-64565111 (Double Blind: JNJ-64565111 5.0 mg)	gnukrwrnyf(bpuczuitrm) = vivhlcsjpf mkruuxgezc (chdqcyumuh, tkgzezdtpj - vfcbcfzglw) View more
NCT03586830 (CTgov)	Phase 2	Type 2 diabetes mellitus in obese	196	Placebo	crxsqsjloz(ikkwfhphdi) = pvzqpihnnj kvqsfrasck (hpfmsamhoj, lqplcleyqy - rfczfdknmk) View more	-	07 Jan 2020