Delving into the Latest Updates on Sitagliptin Phosphate with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Glactiv, Sitagliptin phosphate (USAN), Sitagliptin Phosphate Hydrate

+ [20]

Target

DPP-4

Action

inhibitors

Mechanism

DPP-4 inhibitors(Dipeptidyl peptidase IV inhibitors)

Therapeutic Areas

Endocrinology and Metabolic DiseaseSkin and Musculoskeletal DiseasesOther Diseases

Active Indication

Diabetes Mellitus, Type 2Phobia, SocialOsteoporosis

Inactive Indication

Diabetes Mellitus, Type 1Diabetes, GestationalGastroparesis+ [11]

Originator Organization

Merck Sharp & Dohme Corp.

Active Organization

Ono Pharmaceutical Co., Ltd.

Friedrich Alexander Universität Erlangen NürnbergMerck Sharp & Dohme BV

+ [5]

Inactive Organization

GSK Plc

Takeda Pharmaceutical Co., Ltd.

License Organization

Ono Pharmaceutical Co., Ltd.

Merck & Co., Inc.

Almirall SA

Drug Highest PhaseApproved

First Approval Date

United States (16 Oct 2006),

Diabetes Mellitus, Type 2

RegulationPriority Review (China)

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Structure/Sequence

Molecular FormulaC16H20F6N5O6P

InChIKeyGQPYTJVDPQTBQC-KLQYNRQASA-N

CAS Registry654671-77-9

Disproportionality analyses, including the reporting odds ratio (ROR), the proportional reporting ratio (PRR), the Bayesian confidence propagation neural network (BCPNN), and the multi- item gamma Poisson shrinker (MGPS) algorithms, were employed to quantify the signals of SGLT-2i-associated musculoskeletal and connective tissue disorders AEs.

RESULTS:

The search retrieved a total of 3,206 cases of musculoskeletal and connective tissue disorder-related AEs during the reporting period. This included 1,061 cases for Canagliflozin, 1,052 cases for Dapagliflozin, 1,074 cases for Empagliflozin, and 19 cases for Ertugliflozin. Fifteen preferred terms (PTs) with significant disproportionality were retained. No musculoskeletal and connective tissue system-related AE signals were reported for Ertugliflozin. We identified a risk of muscle necrosis with Canagliflozin use, a risk of sarcopenia with Dapagliflozin use, and a chance of muscle atrophy with Dapagliflozin and Empagliflozin prescriptions. Most cases occurred within the first month after SGLT-2i initiation, and AEs can persist beyond 360 days of use.

CONCLUSIONS:

Our study identified potential new musculoskeletal and connective tissue disorder-related AE signals associated with SGLT-2 inhibitors.

01 Jan 2026·LUMINESCENCE

Simple and Novel Fluorimetric Protocol for Sitagliptin Estimation Through Sensitivity Enhancement Using Acetic Acid: Application to Pharmaceutical Dosage Form With Green Assessment

Article

Author: Shahin, Reem Y. ; Noureldeen, Deena A. M. ; Attia, Tamer Z. ; Taha, Hager M.

ABSTRACT:

A simple, cost‐effective, reproducible, highly sensitive, and green spectrofluorimetric technique for sitagliptin phosphate estimation has been established in its pure form and commercial formulation. The native fluorescence of sitagliptin was enhanced by inhibiting photoinduced electron transfer through optimization of medium pH. The highest fluorescence intensity of sitagliptin was observed at 296 and 583 nm after excitation at 265 nm, using 0.50‐M acetic acid. The method exhibited a wide linearity range (0.30–4.00 μg/mL) with high correlation coefficient values of 0.9998 at both 296 and 583 nm, limits of detection of 0.09 and 0.10 μg/mL, and the limits of quantitation of 0.27 and 0.29 μg/mL, respectively. The guidelines of ICH have been applied for validation of the proposed method. The obtained results have been compared with the previous reported methods. The developed fluorimetric protocol demonstrated high accuracy and excellent precision for estimation of sitagliptin in commercial tablets. Furthermore, the method was confirmed to be environmentally friendly using AGREE, GAPI, Analytical Eco‐Scale, MA, and AGSA tools. As a conclusion, the proposed fluorimetric protocol is highly suitable for the quality control of sitagliptin phosphate.

01 Jan 2026·BIOMEDICAL CHROMATOGRAPHY

From Separation to Safety Prediction: Validated RP‐HPLC Method for Simultaneous Estimation of Sitagliptin and Lobeglitazone, LC‐MS/MS Identification of Degradant Products, and In Silico Safety Profiling

Article

Author: Patel, Rutvi ; Prajapati, Viraj ; Shah, Kushal ; Thummar, Kashyap ; Panchal, Gaurav ; Moradia, Akshita

ABSTRACT:

Diabetes mellitus is a global health burden, necessitating effective combination therapies. The fixed‐dose formulation of sitagliptin phosphate (SGP, 100 mg) and lobeglitazone sulfate (LGS, 0.5 mg) offers synergistic benefits by enhancing insulin sensitivity and glucose‐dependent insulin secretion. However, simultaneous quantification remains challenging due to their dosage disparity and the narrow therapeutic index of LGS. This study reports a validated, stability‐indicating RP‐HPLC method for concurrent estimation of SGP and LGS in a synthetic mixture. Separation was achieved on a Pursuit 5 Diphenyl column (150 × 4.6 mm, 5 μm) using a gradient of 0.1% formic acid and acetonitrile at 1.0 mL/min, with PDA detection at 254 nm. The method complied with ICH Q2(R2) guidelines, showing specificity, linearity, accuracy, precision, and robustness. Forced degradation studies revealed marked instability of SGP under acidic and alkaline conditions, whereas LGS remained stable. LC‐MS/MS analysis identified a major degradation product at m / z 234, and probable fragmentation pathways were proposed. In silico ADMET and toxicity profiling predicted high gastrointestinal absorption for all degradation products, with PI‐1 and PI‐2 flagged for carcinogenicity and all except PI‐3 showing nephrotoxicity. This integrated analytical–computational approach provides a reliable tool for quality control and safety assessment of this antidiabetic formulation.

128

News (Medical) associated with Sitagliptin Phosphate

27 Jan 2026

·www.biospace.com

StarkAge Therapeutics Announces Research Collaboration with Gustave Roussy to Advance Senolytic Therapies in Digestive Cancers

PRESS RELEASE StarkAge Therapeutics Announces Research Collaboration with Gustave Roussy to Advance Senolytic Therapies in Digestive Cancers The collaboration will inform patient selection for treatment with STX-1, a first-in-class senolytic ADC directed against dipeptidyl-peptidase 4 (DPP4/CD26) as it progresses toward IND-enabling studies. Lille, France, January 27th, 2025 – StarkAge Therapeutics, a biotechnology company developing first-in-class senolytic antibody-drug conjugates (ADC) in age-related diseases, with an initial focus on oncology, today announced a research collaboration with Gustave Roussy, Europe’s leading cancer center. The program is dedicated to characterize cellular senescence induced by standard of care (SoC) treatments in a large series of digestive cancers. The result will inform the clinical development of STX-01, a first-in-class senolytic ADC targeting DDP4, a specific marker of senescence, frequently constitutively expressed on primary tumors and/or overexpressed in metastases. Benjamin Le Calvé, Chief Executive Officer of StarkAge Therapeutics , and Eric Angevin, Chief Medical Officer , commented: “This collaboration with Gustave Roussy is an important step as we move forward to IND-enabling studies. Gustave Roussy has an exceptional expertise in digestive cancers, pathology and computational biology and the results will help us enrich the positioning of STX-1 and accelerate the development of senescence-targeted therapies for patients with high medical need.” Antoine Hollebecque, MD, Gastrointestinal cancers at the Department of drug development (DITEP) at Gustave Roussy , added: “Senescence is induced by certain anticancer treatments, and accumulation of senescent cells within tumors significantly reduces patient survival. This collaboration with StarkAge will generate high-resolution biological insights and could open new therapeutic avenues to eliminate both senescent and malignant cells in refractory cancer patients.” Conducted under a research agreement with Gustave Roussy and its technology transfer affiliate, Gustave Roussy Transfert , this collaboration will combine StarkAge’s expertise in senescence biology with Gustave Roussy’s world-class capabilities in multiplexed pathology, and computational oncology. About senescence and cancer Although they no longer divide and have ceased to exercise their original function, senescent cells accumulate in aged or diseased tissues and release pro-inflammatory molecules that contribute to the development of numerous associated pathologies such as cancers, neurodegenerative diseases, fibroses (renal, cardiac, pulmonary, and hepatic), and skeletal pathologies such as osteoarthritis. In cancers, many treatments, including chemotherapy, radiotherapy, and targeted therapies, are known to induce senescence of cancer cells, contributing to drug resistance, metastatic dissemination, and local immunosuppression. Accumulation of senescent cells within tumors is strongly associated with poorer outcomes, significantly reducing patient survival. About DPP4 and STX-1 StarkAge has identified DPP4 (CD26), a highly selective marker of cellular senescence and a relevant tumor-associated antigen, leading to the development of proprietary monoclonal antibodies. STX-1 is a first-in-class DPP4-targeted ADC, currently in preclinical development. END About StarkAge Therapeutics StarkAge Therapeutics is a biotechnology company based in Lille, France, developing first-in-class senolytic antibody–drug conjugates (ADCs) to address age-related diseases, with an initial focus on oncology. The company’s lead program, STX-1, is a first-in-class ADC targeting DPP4, a highly selective marker of cellular senescence and a relevant tumor-associated antigen. STX-1 is currently progressing toward IND-enabling studies. About Gustave Roussy Ranked first in France, first in Europe and sixth in the world, Gustave Roussy is a centre of global expertise entirely dedicated to patients living with cancer. The Institute is a founding pillar of the Paris Saclay Cancer Cluster. Source of therapeutic innovations and diagnostic breakthroughs, the Institute welcomes nearly 50,000 patients each year, including 3,500 children and adolescents, and develops an integrated approach combining research, care and teaching. An expert in rare cancers and complex tumours, Gustave Roussy treats all cancers at all stages of life. It offers its patients personalised care that combines innovation and humanity, taking into account both care and the physical, psychological and social quality of life. With 4,100 employees at two sites, Villejuif and Chevilly-Larue, Gustave Roussy brings together the expertise essential for high-level cancer research; 32% of treated patients are included in clinical studies. To find out more about Gustave Roussy and follow the Institute’s news: , X , Facebook , LinkedIn , Instagram and Bluesky . Media Contacts StarkAge Therapeutics Marie Puvieux – Press Officer, ATCG Partners Starkage@atcg-partners.com +33 610 54 36 72 Gustave Roussy / Gustave Roussy Transfert Claire Parisel and Leona Pinto presse@gustaveroussy.fr +33 142 11 63 59 | +33 142 11 50 59 | +33 617 66 00 26 Attachment PR in English

ADC

05 Jan 2026

·pmlive.com

Merck announces agreement with US government to reduce prices of prescription medication

Merck (known as MSD outside the US) has announced an agreement with the US government to provide key products to patients at affordable prices. Merck plans to establish a direct-to-patient programme that would offer certain medication to eligible patients at affordable prices, including Januvia, Janumet and Janumet XR. Through the programme, Januvia, Janumet and Janumet XR will be available to eligible US patients at a cash price that is approximately 70% less than the current list price. Upon FDA approval, the list will be expanded to include enlicitide, an oral drug candidate designed to lower LDL cholesterol. The agreement means that US pharmaceutical tariffs on the company will be delayed for three years. The announcement comes as part of Merck’s commitment to expand its innovation and manufacturing presence in the US. Merck currently has 15 manufacturing and R&D facilities employing over 30,000 people in the US. Since 2017, it has invested over $12bn in US manufacturing, and since 2018 it has invested $81bn in US R&D. Over the coming years, Merck plans to invest over $70bn in US capital and R&D spending, including at least $12bn in capital expenditures. This includes the recently announced manufacturing facilities in Virginia, Kansas and Delaware, creating 1,200 full-time jobs and supporting 15,000 construction jobs. Robert M Davis, chairman and CEO of Merck, said: “[This] agreement marks a pivotal step in ensuring Americans can access medicines they need at lower costs. “For too long, global pricing imbalances have shifted the financial burden of groundbreaking research and development onto the US healthcare system and ultimately, American patients.”

30 Dec 2025

·firstwordpharma.com

'Threadbare administrative record': Federal judge stops 340B rebate pilot

Just days before the US Health Resources and Services Administration (HRSA) was set to launch a pilot evaluating a rebate-based model of the 340B discount programme, its rollout has been blocked by a federal judge.The American Hospital Association (AHA), along with the Maine Hospital Association and four safety-net hospitals, filed suit at the beginning of December to block the pilot's Jan. 1, 2026 launch, arguing that a rebate system "would inflict hundreds of millions of dollars’ worth of annual costs on hospitals." Judge Lance Walker of the US District Court for the District of Maine sided with the plaintiffs on Monday, issuing an injunction against the pilot as its "economic impact and disruption to services is substantial and… sufficient to demonstrate irreparable injury."Rebate pushCurrently, 340B-eligible hospitals — which serve uninsured and low-income patients — receive significant discounts on drugs upfront, but drugmakers have argued that the programme is rife with abuse, and that large hospital systems exploit the discounts by inflating prices for both uninsured patients and insurers. And for drugs set to debut lower Medicare prices next year thanks to negotiations under the Inflation Reduction Act (IRA), pharmaceutical companies are concerned their products may be subjected to duplicative price concessions if they are also purchased at the 340B price. To avoid potential abuse and "double-dipping," several pharmas, including Johnson & Johnson, Eli Lilly and Bristol Myers Squibb have pushed to adopt a model where hospitals would be required to pay the full amount of a drug upfront, then file for a rebate afterwards. Though their efforts to move to a rebate model were initially rebuffed, HRSA announced in July it would launch a pilot programme "to test…in a methodical and thoughtful approach…a fair and transparent 340B rebate model process." In October, nine therapeutics were accepted for the pilot, including three from J&J: Stelara (ustekinumab), an IL-12/IL-23 inhibitor approved for several autoimmune diseases; oral anticoagulant Xarelto (rivaroxaban); and blood cancer treatment Imbruvica (ibrutinib), which it co-commercialises with AbbVie. Other pilot participants include BMS's anticoagulant Eliquis (apixaban), Boehringer Ingelheim and Eli Lilly's diabetes and heart failure treatment Jardiance (empagliflozin), Merck & Co.'s diabetes drug Januvia (sitagliptin), Novo Nordisk's NovoLog family of insulin products, AstraZeneca's diabetes drug Farxiga (dapagliflozin), and Amgen's Enbrel (etanercept), which is used to treat chronic inflammatory diseases such as rheumatoid arthritis, psoriasis, psoriatic arthritis, ankylosing spondylitis and juvenile idiopathic arthritis. Each product selected for the 340B rebate model pilot was also part of the first round of Medicare price negotiations, which is also set to go into effect on Jan. 1, 2026.'Fatal' errorWhile the Administrative Procedure Act (APA) provides a pathway for US agencies to launch new programmes, it requires that the same be "reasonable and reasonably explained," with an agency tasked with keeping a "record of the relevant factors it considered and…a reasoned explanation for its course of action."However, Walker found that HRSA's rebate pilot did not meet these "vanishingly minimal requirements.""The Agency’s roll out has involved a rather threadbare administrative record that likely fails to consider and reasonably explain the impact of a rebate model on 340B hospitals, who rely on upfront price concessions to stretch few resources as far as possible to serve rural and poor communities," he wrote in his ruling. In the suit, AHA claimed that a rebate model would "impose vast administrative costs to submit, track, recover, and potentially dispute the rebates," while also draining hospitals "of huge sums of money through payments to drug companies that the hospitals then must wait to have refunded," and which drugmakers "have every incentive to slow and stymie the issuance of rebates." Walker took issue with the fact that HRSA is still evaluating administrative costs of its pilot. "This failure to consider administrative costs before approving the manufacturers’ applications under the Rebate Program is fatal under the APA," he concluded. "Defendants cannot fly the plane before they build it."

AHA

100 Deals associated with Sitagliptin Phosphate

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External Link

KEGG	Wiki	ATC	Drug Bank
D06645	Sitagliptin Phosphate	A10BH01	DB01261

R&D Status

Approved

10 top approved records.

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Indication	Country/Location	Organization	Date
Diabetes Mellitus, Type 2	United States	Merck Sharp & Dohme Corp.	16 Oct 2006

Developing

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Inflammation	Phase 3	Canada	Merck Sharp & Dohme Corp.	01 Aug 2015
Hypoglycemia	Phase 3	-	Merck Sharp & Dohme Corp.	22 Jun 2010
Hyperlipidemias	Phase 3	Canada	Merck Sharp & Dohme Corp.	01 Feb 2008
Kidney Failure, Chronic	Phase 3	-	Merck Sharp & Dohme Corp.	19 Oct 2007
Diabetes, Gestational	Phase 2	Italy	Merck Sharp & Dohme Corp.	01 May 2011
Insulin Resistance	Phase 2	Italy	Merck Sharp & Dohme Corp.	01 May 2011
Prediabetic State	Phase 2	Italy	Merck Sharp & Dohme Corp.	01 May 2011
Type 2 diabetes mellitus with established diabetic nephropathy	Phase 2	United States	GSK Plc	05 Jun 2009
Glucose Intolerance	Phase 2	United States	Merck Sharp & Dohme Corp.	01 Mar 2009
Heart Failure	Phase 1	United States	Merck Sharp & Dohme Corp.	01 Apr 2008

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT06770894 (SLowDOWN, Pubmed \| BMC Med)	Phase 3	Diabetes Mellitus, Type 2	132	Sitagliptin	dgfcwyksrm(xeqejvonzi): Difference = 0.11 (95.0% CI, 0.03 - 0.19), P-Value = 0.0063 View more	Positive	14 Oct 2025
				Placebo
NCT03738878 (CTgov)	Phase 4	Hypertension \| Essential Hypertension	4	LCZ696 (LCZ696)	kkcgeqnxwn(ytiyvpukwf) = viammqfryf tycbtzujir (odlyuelpkp, fjftwyckzw - rgviqadnry)	-	03 Aug 2025
				Valsartan (Valsartan)	kkcgeqnxwn(ytiyvpukwf) = mkoxttqevo tycbtzujir (odlyuelpkp, zdvgxsrkyg - oyfrdpvozu) View more
ChiCTR2000039424 (Pubmed) Manual	Phase 4	Diabetes Mellitus, Type 2	701	Metformin combined with Acarbose 100 mg	dzlbwdwqok(zvkxcslcxt) = hgxpxtvccw bgirpqmwbh (bsgacyccov ) View more	Positive	05 May 2025
				Metformin combined with Sitagliptin 100 mg	dzlbwdwqok(zvkxcslcxt) = ffvplnunjm bgirpqmwbh (bsgacyccov ) View more
NCT01794143 (Pubmed \| PLoS One)	Phase 3	Diabetes Mellitus, Type 2	-	Glargine	lwkothnoth(rcfcvudvcb) = cbwdfnivrf laaivhwsim (zwkakdruhi ) View more	Positive	15 Nov 2024
				Glimepiride	lwkothnoth(rcfcvudvcb) = koazozkpac laaivhwsim (zwkakdruhi ) View more
NCT01794143 (GRADE, Pubmed \| J Diabetes Complications)	Phase 3	Diabetes Mellitus	4,098	Glargine	mgvfvhseys(zihpvzqoij) = kpuxkfqzxv ebxzidbgre (mtejbwazvu )	Positive	01 Mar 2024
				Glimepiride	mgvfvhseys(zihpvzqoij) = irwrdlosgi ebxzidbgre (mtejbwazvu )
DIVERSITY-CVR (EASD2023)	Not Applicable	Diabetes Mellitus, Type 2	340	Sitagliptin	otuqnztfpf(cosfvvggpr) = kxwywuwofy uvufpphfnj (nwjtjakaps ) View more	Positive	04 Oct 2023
				Dapagliflozin	otuqnztfpf(cosfvvggpr) = ajarkffrdd uvufpphfnj (nwjtjakaps ) View more
NCT02653209 (TriMaster, Pubmed \| Nat Med)	Phase 4	Diabetes Mellitus, Type 2 Third line	448	Pioglitazone 30mg	yqhrpjbqqo(bmqttbxbxk) = bsqnvneqgx upghfbnlng (zywinixpuy )	-	01 Feb 2023
				Sitagliptin 100mg	yqhrpjbqqo(bmqttbxbxk) = xhucvhatqd upghfbnlng (zywinixpuy )
NCT01794143 (GRADE, Pubmed \| N Engl J Med)	Phase 3	Diabetes Mellitus, Type 2	5,047	Insulin glargine U-100	gzwyugilbg(tkitkolxfr): HR = 0.7 (95% CI, 0.6 - 0.9)	-	22 Sep 2022
				Liraglutide
NCT00659711 (1928, CTgov)	Not Applicable	Type 2 diabetes mellitus in obese	22	Januvia (Sitagliptin) 100 mg (Januvia 100mg)	ppxbrwzypo(yebqeaubtc) = thwvqiqraq jragjxmxot (ilhekqcoig, 10) View more	-	21 Jul 2022
				Placebo (Placebo)	ppxbrwzypo(yebqeaubtc) = pjewxqbecy jragjxmxot (ilhekqcoig, 8) View more
NCT01879228 (CTgov)	Not Applicable	Cystic Fibrosis \| Exocrine Pancreatic Insufficiency	26	Sitagliptin (Sitagliptin)	dlxtekdgsu(zeeoyyutqg) = spynmnnggu qeyecowvzg (hphutjocnn, wgfhdooujj - tsblsvirky) View more	-	09 Feb 2022
				Placebo (Placebo)	dlxtekdgsu(zeeoyyutqg) = jaudjealqp qeyecowvzg (hphutjocnn, qzjsiabwot - bdabfksenp) View more