DAPAGLIFLOZIN; METFORMIN HYDROCHLORIDE; SAXAGLIPTIN HYDROCHLORIDE - Generic Drug Details

What are the generic drug sources for dapagliflozin; metformin hydrochloride; saxagliptin hydrochloride and what is the scope of freedom to operate?

Dapagliflozin; metformin hydrochloride; saxagliptin hydrochloride is the generic ingredient in one branded drug marketed by Astrazeneca Ab and is included in one NDA. There are six patents protecting this compound. Additional information is available in the individual branded drug profile pages.

Dapagliflozin; metformin hydrochloride; saxagliptin hydrochloride has three hundred and forty-six patent family members in forty-eight countries.

Summary for DAPAGLIFLOZIN; METFORMIN HYDROCHLORIDE; SAXAGLIPTIN HYDROCHLORIDE

International Patents:	346
US Patents:	6
Tradenames:	1
Applicants:	1
NDAs:	1
Clinical Trials:	19
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for DAPAGLIFLOZIN; METFORMIN HYDROCHLORIDE; SAXAGLIPTIN HYDROCHLORIDE
DailyMed Link:	DAPAGLIFLOZIN; METFORMIN HYDROCHLORIDE; SAXAGLIPTIN HYDROCHLORIDE at DailyMed

DrugPatentWatch^® Estimated Loss of Exclusivity (LOE) Date for DAPAGLIFLOZIN; METFORMIN HYDROCHLORIDE; SAXAGLIPTIN HYDROCHLORIDE

Dosage:

TABLET, EXTENDED RELEASE;ORAL

^*The generic entry opportunity date is the latter of the last compound-claiming patent and the last regulatory exclusivity protection. Many factors can influence early or later generic entry. This date is provided as a rough estimate of generic entry potential and should not be used as an independent source.

Recent Clinical Trials for DAPAGLIFLOZIN; METFORMIN HYDROCHLORIDE; SAXAGLIPTIN HYDROCHLORIDE

Identify potential brand extensions & 505(b)(2) entrants

Sponsor	Phase
Sabyasachi Sen	Phase 4
Shenzhen Sixth People's Hospital	Phase 4
Dongguan Kanghua Hospital	Phase 4

See all DAPAGLIFLOZIN; METFORMIN HYDROCHLORIDE; SAXAGLIPTIN HYDROCHLORIDE clinical trials

Anatomical Therapeutic Chemical (ATC) Classes for DAPAGLIFLOZIN; METFORMIN HYDROCHLORIDE; SAXAGLIPTIN HYDROCHLORIDE

A10BA	Biguanides
A10B	BLOOD GLUCOSE LOWERING DRUGS, EXCL. INSULINS
A10	DRUGS USED IN DIABETES
A	Alimentary tract and metabolism

A10BH	Dipeptidyl peptidase 4 (DPP-4) inhibitors
A10B	BLOOD GLUCOSE LOWERING DRUGS, EXCL. INSULINS
A10	DRUGS USED IN DIABETES
A	Alimentary tract and metabolism

A10BK	Sodium-glucose co-transporter 2 (SGLT2) inhibitors
A10B	BLOOD GLUCOSE LOWERING DRUGS, EXCL. INSULINS
A10	DRUGS USED IN DIABETES
A	Alimentary tract and metabolism

US Patents and Regulatory Information for DAPAGLIFLOZIN; METFORMIN HYDROCHLORIDE; SAXAGLIPTIN HYDROCHLORIDE

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Exclusivity Expiration
Astrazeneca Ab	QTERNMET XR	dapagliflozin; metformin hydrochloride; saxagliptin hydrochloride	TABLET, EXTENDED RELEASE;ORAL	210874-003	May 2, 2019		DISCN	Yes	No				Y
Astrazeneca Ab	QTERNMET XR	dapagliflozin; metformin hydrochloride; saxagliptin hydrochloride	TABLET, EXTENDED RELEASE;ORAL	210874-003	May 2, 2019		DISCN	Yes	No			Y	Y
Astrazeneca Ab	QTERNMET XR	dapagliflozin; metformin hydrochloride; saxagliptin hydrochloride	TABLET, EXTENDED RELEASE;ORAL	210874-001	May 2, 2019		DISCN	Yes	No			Y
Astrazeneca Ab	QTERNMET XR	dapagliflozin; metformin hydrochloride; saxagliptin hydrochloride	TABLET, EXTENDED RELEASE;ORAL	210874-004	May 2, 2019		DISCN	Yes	No			Y
Astrazeneca Ab	QTERNMET XR	dapagliflozin; metformin hydrochloride; saxagliptin hydrochloride	TABLET, EXTENDED RELEASE;ORAL	210874-003	May 2, 2019		DISCN	Yes	No			Y

Expired US Patents for DAPAGLIFLOZIN; METFORMIN HYDROCHLORIDE; SAXAGLIPTIN HYDROCHLORIDE

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	Patent No.	Patent Expiration
Astrazeneca Ab	QTERNMET XR	dapagliflozin; metformin hydrochloride; saxagliptin hydrochloride	TABLET, EXTENDED RELEASE;ORAL	210874-003	May 2, 2019
Astrazeneca Ab	QTERNMET XR	dapagliflozin; metformin hydrochloride; saxagliptin hydrochloride	TABLET, EXTENDED RELEASE;ORAL	210874-002	May 2, 2019
Astrazeneca Ab	QTERNMET XR	dapagliflozin; metformin hydrochloride; saxagliptin hydrochloride	TABLET, EXTENDED RELEASE;ORAL	210874-004	May 2, 2019
Astrazeneca Ab	QTERNMET XR	dapagliflozin; metformin hydrochloride; saxagliptin hydrochloride	TABLET, EXTENDED RELEASE;ORAL	210874-004	May 2, 2019
Astrazeneca Ab	QTERNMET XR	dapagliflozin; metformin hydrochloride; saxagliptin hydrochloride	TABLET, EXTENDED RELEASE;ORAL	210874-001	May 2, 2019

International Patents for DAPAGLIFLOZIN; METFORMIN HYDROCHLORIDE; SAXAGLIPTIN HYDROCHLORIDE

Country	Patent Number	Title	Estimated Expiration
New Zealand	574346	CRYSTALLINE SOLVATES AND COMPLEXES OF (IS) -1, 5-ANHYDRO-L-C- (3- ( (PHENYL) METHYL) PHENYL) -D-GLUCITOL DERIVATIVES WITH AMINO ACIDS AS SGLT2 INHIBITORS FOR THE TREATMENT OF DIABETES
Japan	5475636
Malaysia	147639	COATED TABLET FORMULATION AND METHOD
Japan	2018172418	二層錠製剤 (BILAYER TABLET FORMULATIONS)
Brazil	PI0311323	composto inibidor de c-aril glicosídeo sglt2, composição farmacêutica e combinação

Supplementary Protection Certificates for DAPAGLIFLOZIN; METFORMIN HYDROCHLORIDE; SAXAGLIPTIN HYDROCHLORIDE

Patent Number	Supplementary Protection Certificate	SPC Country	SPC Expiration	SPC Description
1506211	PA2014026	Lithuania		PRODUCT NAME: DAPAGLIFOZINUM + METFORMINUM; REGISTRATION NO/DATE: EU/1/13/900 20140116
1506211	PA 2013 008, C 1506211	Lithuania		PRODUCT NAME: DAPAGLIFLOZINUM; REGISTRATION NO/DATE: EU/1/12/795/001 - EU/1/12/795/010 20121112
1506211	C20130006 00074	Estonia		PRODUCT NAME: DAPAGLIFLOZIN;REG NO/DATE: K(2012)8378 12.11.2012
1506211	179 5017-2014	Slovakia		PRODUCT NAME: KOMBINACIA DAPAGLIFLOZINU ALEBO JEHO FARMACEUTICKY PRIJATELNYCH SOLI A METFORMINU ALEBO JEHO FARMACEUTICKY PRIJATELNYCH SOLI; REGISTRATION NO/DATE: EU/1/13/900/001 - EU/1/13/900/012 20140116
1506211	C300677	Netherlands		PRODUCT NAME: COMBINATIE VAN DAPAGLIFLOZINE OF EEN FARMACEUTISCH AANVAARDBAAR ZOUT DAARVAN EN METFORMINE OF EEN FARMACEITISCH AANVAARDBAAR ZOUT DAARVAN, ZOALS BESCHERMD DOOR HET BASISOCTROOI EP 1506211B1; REGISTRATION NO/DATE: EU/1/13/900 20140121

DAPAGLIFLOZIN; METFORMIN HYDROCHLORIDE; SAXAGLIPTIN HYDROCHLORIDE Market Analysis and Financial Projection Experimental

Market Dynamics and Financial Trajectory for Dapagliflozin, Metformin Hydrochloride, and Saxagliptin Hydrochloride

Introduction

The diabetes treatment market is highly competitive and dynamic, with various medications vying for market share. Dapagliflozin, metformin hydrochloride, and saxagliptin hydrochloride are key players in this market, each offering unique benefits and challenges. Here, we delve into the market dynamics and financial trajectory of these drugs.

Market Landscape

Competitive Environment

The diabetes treatment market is crowded with various classes of drugs, including SGLT2 inhibitors, DPP-4 inhibitors, and biguanides. Dapagliflozin, an SGLT2 inhibitor, and saxagliptin, a DPP-4 inhibitor, compete directly in this space. Metformin hydrochloride, a biguanide, is often used as a first-line treatment and is frequently combined with other drugs like dapagliflozin and saxagliptin[3].

Unique Selling Propositions

• Dapagliflozin: Offers significant glycemic control, weight reduction, and blood pressure lowering, making it an attractive option for patients with type 2 diabetes (T2D)[4].
• Metformin Hydrochloride: As a first-line treatment, it is widely prescribed due to its efficacy in lowering blood glucose levels. When combined with dapagliflozin, it forms a unique fixed-dose combination like XIGDUO XR, enhancing its appeal[3].
• Saxagliptin: Known for its safety profile and efficacy in reducing HbA1c levels, saxagliptin is often preferred for its minimal risk of hypoglycemia compared to other oral antidiabetic drugs[5].

Regulatory Environment

Approvals and Expansions

• XIGDUO XR: This fixed-dose combination of dapagliflozin and metformin hydrochloride has been approved in several regions, including the US since 2014 and China in June 2023. These approvals have significantly expanded its market reach[3].
• Global Presence: Dapagliflozin and saxagliptin have received approvals in various countries, allowing them to be prescribed globally. Regulatory approvals are crucial for market penetration and revenue growth.

Financial Trajectory

Revenue Growth

• AstraZeneca's Diabetes Portfolio: Dapagliflozin, under the trade name Farxiga, has seen a 40% increase in revenue in the first half of 2023. XIGDUO XR, which includes dapagliflozin and metformin, contributes to this growth, particularly in emerging markets like China[3].
• Market Share: The unique combination of dapagliflozin and metformin in XIGDUO XR has helped it gain a significant market share in the US and other regions. This combination is expected to drive further growth, especially in China, where type 2 diabetes is prevalent[3].

Geographical Performance

• United States: XIGDUO XR has been part of AstraZeneca's diabetes portfolio in the US since its approval in 2014, contributing to the company's revenue growth in this market[3].
• China and Emerging Markets: The recent approval in China and strong performance in ex-China emerging markets have opened up new revenue streams. The large patient population in China and the drug's first-line treatment status are expected to drive significant growth[3].

Cost-Effectiveness

• Cost-Utility Analysis: Studies have shown that while dapagliflozin and saxagliptin both offer cost-effective options, dapagliflozin tends to be more cost-effective in the long term, especially when considering quality-adjusted life-years (QALYs)[2].
• Pharmacoeconomic Analysis: The combination of dapagliflozin and saxagliptin, while providing additional benefits, comes with a higher total cost. However, dapagliflozin alone often presents a better incremental cost-effectiveness ratio compared to saxagliptin or the combination[2].

Efficacy and Safety

Clinical Outcomes

• Dapagliflozin: Demonstrates greater glycemic efficacy, weight reduction, and blood pressure lowering compared to saxagliptin. It also has a favorable safety profile with lower incidence of hypoglycemia[1][4].
• Saxagliptin: Offers similar efficacy to other DPP-4 inhibitors and is known for its better safety profile, particularly in terms of adverse events and hypoglycemia risk[5].

Patient Outcomes

• Composite Endpoints: Studies have shown that more patients treated with dapagliflozin achieve composite endpoints such as HbA1c reduction, weight loss, and blood pressure reduction without major or minor hypoglycemia compared to saxagliptin[4].

Key Takeaways

• Unique Combinations: The fixed-dose combination of dapagliflozin and metformin hydrochloride in XIGDUO XR sets it apart in the market.
• Global Approvals: Approvals in multiple regions, including the US and China, have expanded the market reach of these drugs.
• Revenue Contribution: These drugs contribute significantly to AstraZeneca's revenue growth, particularly in the diabetes segment.
• Future Growth: The approval in China and other emerging markets is expected to drive further growth, especially for XIGDUO XR.

FAQs

What is the unique selling proposition of XIGDUO XR?

XIGDUO XR offers a unique combination of the SGLT2 inhibitor dapagliflozin and metformin hydrochloride extended-release, providing comprehensive glycemic control and setting it apart in the diabetes treatment market[3].

How does dapagliflozin compare to saxagliptin in terms of glycemic control?

Dapagliflozin demonstrates greater glycemic efficacy than saxagliptin, with additional benefits on weight and systolic blood pressure reduction[1][4].

What is the cost-effectiveness of dapagliflozin and saxagliptin?

Dapagliflozin tends to be more cost-effective in the long term, especially when considering QALYs, although the combination of dapagliflozin and saxagliptin provides additional benefits at a higher total cost[2].

What are the regulatory milestones for XIGDUO XR?

XIGDUO XR has been approved in the US since 2014 and recently in China in June 2023, marking significant milestones in its market expansion[3].

How does the safety profile of saxagliptin compare to other oral antidiabetic drugs?

Saxagliptin has a better safety profile compared to other oral antidiabetic drugs, with a lower incidence of overall adverse events and hypoglycemia[5].

Sources

1. Frias, J. P., et al. "Dapagliflozin plus Saxagliptin Add-On vs. Glimepiride Add-On to Metformin in Patients with Type 2 Diabetes: A Randomized, Double-Blind, 52-Week Trial." Diabetes, vol. 67, no. Supplement 1, 2018.
2. Cost-Utility Analysis of Dapagliflozin Versus Saxagliptin Treatment in Patients with Type 2 Diabetes Mellitus Inadequately Controlled by Metformin. PubMed, 2020.
3. XIGDUO XR Drug Patent Profile. Drug Patent Watch, 2023.
4. Dapagliflozin versus Saxagliptin as Add-On Therapy in Patients with Type 2 Diabetes Inadequately Controlled with Metformin. AEM-SBEM, 2023.
5. Efficacy and Safety of Saxagliptin in Patients with Type 2 Diabetes. PLOS ONE, 2018.