ERTUGLIFLOZIN; SITAGLIPTIN PHOSPHATE - Generic Drug Details

What are the generic sources for ertugliflozin; sitagliptin phosphate and what is the scope of patent protection?

Ertugliflozin; sitagliptin phosphate is the generic ingredient in one branded drug marketed by Msd Sub Merck and is included in one NDA. There are four patents protecting this compound. Additional information is available in the individual branded drug profile pages.

Ertugliflozin; sitagliptin phosphate has one hundred and thirty-eight patent family members in fifty-two countries.

One supplier is listed for this compound.

Summary for ERTUGLIFLOZIN; SITAGLIPTIN PHOSPHATE

International Patents:	138
US Patents:	4
Tradenames:	1
Applicants:	1
NDAs:	1
Finished Product Suppliers / Packagers:	1
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for ERTUGLIFLOZIN; SITAGLIPTIN PHOSPHATE
DailyMed Link:	ERTUGLIFLOZIN; SITAGLIPTIN PHOSPHATE at DailyMed

DrugPatentWatch^® Estimated Loss of Exclusivity (LOE) Date for ERTUGLIFLOZIN; SITAGLIPTIN PHOSPHATE

Constraining patent/regulatory exclusivity:

9,308,204

Dosage:

TABLET;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.

Pharmacology for ERTUGLIFLOZIN; SITAGLIPTIN PHOSPHATE

Drug Class	Dipeptidyl Peptidase 4 Inhibitor
Mechanism of Action	Dipeptidyl Peptidase 4 Inhibitors

Anatomical Therapeutic Chemical (ATC) Classes for ERTUGLIFLOZIN; SITAGLIPTIN PHOSPHATE

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 ERTUGLIFLOZIN; SITAGLIPTIN PHOSPHATE

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Exclusivity Expiration
Msd Sub Merck	STEGLUJAN	ertugliflozin; sitagliptin phosphate	TABLET;ORAL	209805-001	Dec 19, 2017		RX	Yes	No	7,326,708*PED				Y
Msd Sub Merck	STEGLUJAN	ertugliflozin; sitagliptin phosphate	TABLET;ORAL	209805-001	Dec 19, 2017		RX	Yes	No
Msd Sub Merck	STEGLUJAN	ertugliflozin; sitagliptin phosphate	TABLET;ORAL	209805-001	Dec 19, 2017		RX	Yes	No	8,080,580		Y	Y
Msd Sub Merck	STEGLUJAN	ertugliflozin; sitagliptin phosphate	TABLET;ORAL	209805-002	Dec 19, 2017		RX	Yes	Yes	9,439,901
Msd Sub Merck	STEGLUJAN	ertugliflozin; sitagliptin phosphate	TABLET;ORAL	209805-002	Dec 19, 2017		RX	Yes	Yes	7,326,708*PED				Y
Msd Sub Merck	STEGLUJAN	ertugliflozin; sitagliptin phosphate	TABLET;ORAL	209805-001	Dec 19, 2017		RX	Yes	No	9,308,204		Y

Expired US Patents for ERTUGLIFLOZIN; SITAGLIPTIN PHOSPHATE

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	Patent No.	Patent Expiration
Msd Sub Merck	STEGLUJAN	ertugliflozin; sitagliptin phosphate	TABLET;ORAL	209805-002	Dec 19, 2017	7,078,381
Msd Sub Merck	STEGLUJAN	ertugliflozin; sitagliptin phosphate	TABLET;ORAL	209805-001	Dec 19, 2017	6,890,898
Msd Sub Merck	STEGLUJAN	ertugliflozin; sitagliptin phosphate	TABLET;ORAL	209805-002	Dec 19, 2017	7,459,428
Msd Sub Merck	STEGLUJAN	ertugliflozin; sitagliptin phosphate	TABLET;ORAL	209805-002	Dec 19, 2017	6,890,898
Msd Sub Merck	STEGLUJAN	ertugliflozin; sitagliptin phosphate	TABLET;ORAL	209805-001	Dec 19, 2017	7,459,428
Msd Sub Merck	STEGLUJAN	ertugliflozin; sitagliptin phosphate	TABLET;ORAL	209805-001	Dec 19, 2017	7,078,381

International Patents for ERTUGLIFLOZIN; SITAGLIPTIN PHOSPHATE

Country	Patent Number	Title	Estimated Expiration
Panama	8840801	DERIVAOS DE DIOXA-BICICLO[3.2.1]OCTANO-2,3,4-TRIOL
Cyprus	1106936
African Regional IP Organization (ARIPO)	3099	Dioxa-bicyclo[3.2.1]octane-2,3,4-triol de derivatives
Hong Kong	1193606	二氧雜-雙環 辛烷- -三醇衍生物 (DIOXA-BICYCLO[3.2.1.]OCTANE-2,3,4-TRIOL DERIVATIVES -[321]-234-)
Eurasian Patent Organization	201100266	ДИОКСА-БИЦИКЛО[3.2.1]ОКТАН-2,3,4-ТРИОЛЬНЫЕ ПРОИЗВОДНЫЕ
South Africa	200509933	Phosphoric acid salt of a dipeptidyl peptidase-IV inhibitor

Supplementary Protection Certificates for ERTUGLIFLOZIN; SITAGLIPTIN PHOSPHATE

Patent Number	Supplementary Protection Certificate	SPC Country	SPC Expiration	SPC Description
2334687	C02334687/01	Switzerland		FORMER OWNER: PFIZER INC., US
2334687	2018/028	Ireland		PRODUCT NAME: ERTUGLIFLOZIN, OPTIONALLY AS A CRYSTAL FORM, PARTICULARLY AS A CO-CRYSTAL WITH L-PYROGLUTAMIC ACID, AND SPECIFICALLY AS ERTUGLIFLOZIN L-PYROGLUTAMIC ACID; REGISTRATION NO/DATE: EU/1/18/1267/001 EU/1/18/1267/012 20180321
2334687	2018C/027	Belgium		PRODUCT NAME: ERTUGLIFLOZINE, DESGEWENST IN KRISTALVORM, MET NAME ALS CO-KRISTAL MET L-PYROGLUTAMINEZUUR, EN SPECIFIEK ALS ERTUGLIFLOZIN L-PYROGLUTAMINE ZUUR; AUTHORISATION NUMBER AND DATE: EU/1/18/1267 20180323
2334687	132018000000441	Italy		PRODUCT NAME: ERTUGLIFLOZIN(STEGLATRO); AUTHORISATION NUMBER(S) AND DATE(S): EU/1/18/1267, 20180323
2334687	SPC/GB18/026	United Kingdom		PRODUCT NAME: ERTUGLIFOZIN, OPTIONALLY AS A CRYSTAL FORM, PARTICULARLY AS A CO-CRYSTAL WITH L-PYROGLUTAMIC ACID, AND SPECIFICALLY AS ERTUGLIFOZIN L-PYROGLUTAMIC ACID; REGISTERED: UK EU/1/18/1267/001(NI) 20180321; UK EU/1/18/1267/002(NI) 20180321; UK EU/1/18/1267/003(NI) 20180321; UK EU/1/18/1267/004(NI) 20180321; UK EU/1/18/1267/005(NI) 20180321; UK EU/1/18/1267/006(NI) 20180321; UK PLGB 53095/0064 20180321; UK PLGB 53095/0065 20180321; UK EU/1/18/1267/007(NI) 20180321; UK EU/1/18/1267/008(NI) 20180321; UK EU/1/18/1267/009(NI) 20180321; UK EU/1/18/1267/010(NI) 20180321; UK EU/1/18/1267/011(NI) 20180321; UK EU/1/18/1267/012(NI) 20180321
2334687	PA2018510	Lithuania		PRODUCT NAME: ERTUGLIFLOZINAS, PASIRINKTINAI KAIP KRISTALINE FORMA, YPAC KAIP KO-KRISTALAS SU L-PIROGLUTAMO RUGSTIMI, IR YPAC KAIP ERTUGLIFLOZINO L-PIROGLUTAMO RUGSTIS; REGISTRATION NO/DATE: EU/1/18/1267 20180321

ERTUGLIFLOZIN; SITAGLIPTIN PHOSPHATE Market Analysis and Financial Projection Experimental

Market Dynamics and Financial Trajectory for Ertugliflozin and Sitagliptin Phosphate

Introduction

Ertugliflozin and sitagliptin phosphate are key components in the treatment of type 2 diabetes, particularly when used in combination. This article delves into the market dynamics and financial trajectory of these drugs, highlighting their efficacy, market positioning, and financial performance.

Ertugliflozin: An SGLT-2 Inhibitor

Ertugliflozin is a sodium glucose cotransporter-2 (SGLT-2) inhibitor developed by Pfizer and Merck. It works by blocking glucose reabsorption in the kidneys, thereby lowering plasma glucose levels. This mechanism has been shown to improve glycemic control and reduce the risk of microvascular complications in patients with type 2 diabetes mellitus (T2DM)[2][4].

Market Entry and Approval

Ertugliflozin, marketed as Steglatro, received FDA approval in December 2017 and EU approval in March 2018. It is available as a standalone medication and in fixed-dose combinations with sitagliptin (Steglujan) and metformin (Segluromet)[3][4].

Clinical Efficacy

Clinical trials, including the VERTIS Mono and VERTIS Factorial studies, have demonstrated that ertugliflozin significantly reduces HbA1c levels. When combined with sitagliptin, the efficacy is enhanced, showing greater reductions in HbA1c, fasting plasma glucose (FPG), body weight, and systolic blood pressure compared to either drug alone[4][5].

Safety Profile

While ertugliflozin has shown a favorable safety profile, it is associated with increased risks of genital infections, urinary tract infections, and hypoglycemia. However, combination therapy with sitagliptin and metformin has been generally well-tolerated with no significant toxicities observed[2][5].

Market Positioning

Ertugliflozin entered a crowded SGLT-2 inhibitor market, competing with established drugs like Invokana (canagliflozin) and Farxiga (dapagliflozin). Despite being a late entrant, Steglatro has been predicted to achieve significant market share. The 2018 Drugs to Watch report forecasted Steglatro to reach sales of $1.275 billion by 2022, making it a valuable addition to the rapidly rising SGLT-2 inhibitor market[3].

Financial Performance

The financial trajectory of ertugliflozin is promising, driven by its efficacy and the growing demand for SGLT-2 inhibitors. The market for SGLT-2 inhibitors has seen rapid growth, with Farxiga and Jardiance leading the pack. Steglatro, along with its fixed-dose combinations, is expected to contribute substantially to this growth, with forecasts indicating a significant increase in sales over the coming years[3].

Sitagliptin Phosphate: A DPP-4 Inhibitor

Sitagliptin phosphate, marketed as Januvia, is a dipeptidyl peptidase-4 (DPP-4) inhibitor developed by Merck. It works by inhibiting the breakdown of incretin hormones, thereby increasing insulin release and decreasing glucagon levels in the bloodstream[1][2].

Market Presence

Januvia has been a leading drug in the DPP-4 inhibitor market since its approval in 2006. It is often used in combination with other antidiabetic drugs, including metformin (Janumet) and ertugliflozin (Steglujan)[1].

Combination Therapy with Ertugliflozin

The combination of ertugliflozin and sitagliptin has been shown to be more effective than either drug alone. This combination, marketed as Steglujan, has demonstrated significant reductions in HbA1c, FPG, body weight, and systolic blood pressure. The synergy between these two mechanisms of action enhances glycemic control and provides additional benefits such as weight loss and blood pressure reduction[4][5].

Safety and Tolerability

The combination of ertugliflozin and sitagliptin has been generally well-tolerated. Studies have shown that the safety profile of this combination is consistent with the individual components, with no significant drug-drug interactions observed[2][5].

Financial Impact of Combination Therapy

The financial impact of the combination therapy is substantial. By offering a more effective treatment option, Steglujan and other fixed-dose combinations are likely to capture a larger market share. The enhanced efficacy and safety profile of these combinations contribute to higher patient adherence and satisfaction, which in turn drive sales and revenue[3].

Competitive Landscape

The competitive landscape for SGLT-2 inhibitors and DPP-4 inhibitors is highly dynamic. With multiple players in the market, the competition is fierce. However, the unique combination of ertugliflozin and sitagliptin offers a competitive edge due to its comprehensive benefits in glycemic control, weight management, and cardiovascular risk reduction[3].

Regulatory Environment

Regulatory approvals and guidelines play a crucial role in the market dynamics of these drugs. The FDA and EU approvals for ertugliflozin and its combinations have been pivotal in their market entry. Ongoing regulatory support and updates will continue to influence their financial trajectory[2][3].

Patient and Physician Preferences

Patient and physician preferences are influenced by the efficacy, safety, and convenience of treatment options. The combination of ertugliflozin and sitagliptin offers a convenient once-daily dosing regimen, which enhances patient compliance. Additionally, the comprehensive benefits of this combination make it a preferred choice among physicians[4][5].

Future Outlook

The future outlook for ertugliflozin and sitagliptin phosphate is promising. As the prevalence of type 2 diabetes continues to rise, the demand for effective and safe treatment options will increase. The combination therapy of these drugs is poised to play a significant role in meeting this demand, driving both clinical and financial success.

Key Takeaways

• Ertugliflozin is an SGLT-2 inhibitor that improves glycemic control by blocking glucose reabsorption in the kidneys.
• Sitagliptin phosphate is a DPP-4 inhibitor that enhances insulin release and decreases glucagon levels.
• Combination Therapy: The combination of ertugliflozin and sitagliptin (Steglujan) offers enhanced efficacy and safety compared to individual treatments.
• Market Positioning: Steglatro and its combinations are expected to achieve significant market share in the SGLT-2 inhibitor market.
• Financial Performance: The financial trajectory of these drugs is promising, driven by growing demand and forecasted sales increases.
• Regulatory and Patient Preferences: Regulatory approvals and patient/physician preferences favor the combination therapy due to its comprehensive benefits.

FAQs

What is the mechanism of action of ertugliflozin?

Ertugliflozin works by blocking glucose reabsorption in the kidneys, thereby lowering plasma glucose levels.

How does the combination of ertugliflozin and sitagliptin compare to individual treatments?

The combination of ertugliflozin and sitagliptin is more effective than either drug alone in reducing HbA1c, FPG, body weight, and systolic blood pressure.

What are the common side effects associated with ertugliflozin?

Common side effects include genital infections, urinary tract infections, and hypoglycemia.

What is the market forecast for Steglatro by 2022?

The 2018 Drugs to Watch report forecasted Steglatro to reach sales of $1.275 billion by 2022.

How does the regulatory environment impact the market dynamics of these drugs?

Regulatory approvals and guidelines are crucial for market entry and ongoing support, influencing the financial trajectory of these drugs.

Sources

1. Clarivate: JANUVIA®
2. FDA: 209803Orig1s000 209805Orig1s000 209806Orig1s000
3. Clarivate Analytics: Pfizer and Merck's Steglatro for type 2 diabetes
4. Pfizer: Merck and Pfizer Announce Two Pivotal Phase 3 Studies for Ertugliflozin
5. PubMed: Ertugliflozin plus sitagliptin versus either individual agent over 52 weeks in patients with type 2 diabetes inadequately controlled with metformin