Canagliflozin; metformin hydrochloride - Generic Drug Details

What are the generic sources for canagliflozin; metformin hydrochloride and what is the scope of patent protection?

Canagliflozin; metformin hydrochloride is the generic ingredient in two branded drugs marketed by Janssen Pharms and is included in two NDAs. There are six patents protecting this compound and one Paragraph IV challenge. Additional information is available in the individual branded drug profile pages.

Canagliflozin; metformin hydrochloride has two hundred and sixty-nine patent family members in forty-seven countries.

One supplier is listed for this compound.

Summary for canagliflozin; metformin hydrochloride

International Patents:	269
US Patents:	6
Tradenames:	2
Applicants:	1
NDAs:	2
Finished Product Suppliers / Packagers:	1
Clinical Trials:	50
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for canagliflozin; metformin hydrochloride
DailyMed Link:	canagliflozin; metformin hydrochloride at DailyMed

DrugPatentWatch^® Estimated Loss of Exclusivity (LOE) Date for canagliflozin; metformin hydrochloride

Dosage:

TABLET, EXTENDED RELEASE;ORAL

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.

Recent Clinical Trials for canagliflozin; metformin hydrochloride

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

Sponsor	Phase
Ain Shams University	Phase 1/Phase 2
First Affiliated Hospital Xi'an Jiaotong University	N/A
Johnson & Johnson Private Limited	Phase 4

See all canagliflozin; metformin hydrochloride clinical trials

Pharmacology for canagliflozin; metformin hydrochloride

Drug Class	Biguanide Sodium-Glucose Cotransporter 2 Inhibitor
Mechanism of Action	P-Glycoprotein Inhibitors Sodium-Glucose Transporter 2 Inhibitors

Anatomical Therapeutic Chemical (ATC) Classes for canagliflozin; metformin hydrochloride

A10BA	Biguanides
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

Paragraph IV (Patent) Challenges for CANAGLIFLOZIN; METFORMIN HYDROCHLORIDE

Tradename	Dosage	Ingredient	Strength	NDA	ANDAs Submitted	Submissiondate
INVOKAMET XR	Extended-release Tablets	canagliflozin; metformin hydrochloride	50 mg/500 mg 50 mg/1000 mg 150 mg/500 mg 150 mg/1000 mg	205879	1	2018-11-21
INVOKAMET	Tablets	canagliflozin; metformin hydrochloride	50 mg/500 mg 50 mg/1000 mg 150 mg/500 mg 150 mg/1000 mg	204353	6	2017-03-29

US Patents and Regulatory Information for canagliflozin; metformin hydrochloride

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Exclusivity Expiration
Janssen Pharms	INVOKAMET	canagliflozin; metformin hydrochloride	TABLET;ORAL	204353-004	Aug 8, 2014		RX	Yes	Yes			Y
Janssen Pharms	INVOKAMET	canagliflozin; metformin hydrochloride	TABLET;ORAL	204353-003	Aug 8, 2014		RX	Yes	No			Y	Y
Janssen Pharms	INVOKAMET	canagliflozin; metformin hydrochloride	TABLET;ORAL	204353-003	Aug 8, 2014		RX	Yes	No
Janssen Pharms	INVOKAMET XR	canagliflozin; metformin hydrochloride	TABLET, EXTENDED RELEASE;ORAL	205879-001	Sep 20, 2016		RX	Yes	No

Expired US Patents for canagliflozin; metformin hydrochloride

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	Patent No.	Patent Expiration
Janssen Pharms	INVOKAMET XR	canagliflozin; metformin hydrochloride	TABLET, EXTENDED RELEASE;ORAL	205879-003	Sep 20, 2016
Janssen Pharms	INVOKAMET XR	canagliflozin; metformin hydrochloride	TABLET, EXTENDED RELEASE;ORAL	205879-003	Sep 20, 2016
Janssen Pharms	INVOKAMET	canagliflozin; metformin hydrochloride	TABLET;ORAL	204353-004	Aug 8, 2014
Janssen Pharms	INVOKAMET	canagliflozin; metformin hydrochloride	TABLET;ORAL	204353-001	Aug 8, 2014

International Patents for canagliflozin; metformin hydrochloride

Country	Patent Number	Title	Estimated Expiration
Australia	2004260760	Novel compounds
Taiwan	200637852	Indole derivatives
Eurasian Patent Organization	011025	НОВЫЕ СОЕДИНЕНИЯ (NOVEL COMPOUNDS)
World Intellectual Property Organization (WIPO)	2005012321

Supplementary Protection Certificates for canagliflozin; metformin hydrochloride

Patent Number	Supplementary Protection Certificate	SPC Country	SPC Expiration	SPC Description
1651658	C01651658/01	Switzerland		PRODUCT NAME: CANAGLIFLOZIN; REGISTRATION NO/DATE: SWISSMEDIC-ZULASSUNG 62956 29.01.2014
1651658	2014C/027	Belgium		PRODUCT NAME: CANAGLIFLOZINE; AUTHORISATION NUMBER AND DATE: EU/1/13/884 20131119
1651658	C300670	Netherlands		PRODUCT NAME: CANAGLIFLOZINE; REGISTRATION NO/DATE: EU/1/13/884/001-008 20131118
1651658	29/2014	Austria		PRODUCT NAME: CANAGLIFLOZIN; REGISTRATION NO/DATE: EU/1/13/884 20131115

Canagliflozin; metformin hydrochloride Market Analysis and Financial Projection Experimental

Market Dynamics and Financial Trajectory of Canagliflozin and Metformin Hydrochloride

Introduction

Canagliflozin and metformin hydrochloride are two significant medications in the treatment of type 2 diabetes. Canagliflozin, a sodium-glucose cotransporter 2 (SGLT2) inhibitor, and metformin, a biguanide, are often used in combination to achieve better glycemic control. Here, we will delve into the market dynamics and financial trajectory of these drugs, particularly focusing on their combination therapy.

Market Overview of Antidiabetic Drugs

The market for antidiabetic drugs has seen significant growth over the past decade, driven by the increasing prevalence of type 2 diabetes and the introduction of new-generation drugs. Canagliflozin, one of these new-generation drugs, has been a key player in this market[1].

Canagliflozin: Market Performance

Canagliflozin, marketed under the brand name Invokana, was first approved in 2013. Since its introduction, it has shown steady growth in sales. Here are some key financial metrics:

• Sales Growth: From $0 million in 2012 to $129 million in 2021, canagliflozin has demonstrated robust sales growth. Its combination with metformin has further boosted its market presence[1].
• Combination Therapy: The combination of canagliflozin and metformin, known as Vokanamet, has been particularly successful. This fixed-dose combination (FDC) has been shown to be effective and well-tolerated, contributing significantly to the overall sales of canagliflozin[4].

Metformin: A Long-Standing Market Presence

Metformin, one of the oldest and most widely used antidiabetic drugs, continues to be a staple in diabetes treatment.

• Sales Stability: Despite the introduction of new drugs, metformin has maintained a stable market presence. Its sales have fluctuated slightly over the years but remain substantial, with $78 million in sales in 2021[1].
• Combination Benefits: When combined with canagliflozin, metformin enhances the therapeutic efficacy, leading to better glycemic control and additional benefits such as weight reduction[4].

Combination Therapy: Canagliflozin and Metformin

The combination of canagliflozin and metformin has been a strategic move to leverage the strengths of both drugs.

• Clinical Efficacy: Studies have shown that the combination of canagliflozin and metformin extended release (XR) results in significant reductions in A1C levels compared to monotherapy with either drug. This combination also leads to greater weight reduction and is generally well-tolerated[4].
• Market Impact: The approval and launch of this combination therapy have expanded the market reach for both drugs. It has attracted patients who require more effective glycemic control and has helped in retaining market share against other antidiabetic medications.

Regulatory and Clinical Considerations

The regulatory approval process for the combination therapy involved rigorous clinical trials and pharmacokinetic studies.

• Dosing Regimens: The FDA approved the fixed-dose combination of canagliflozin and metformin after evaluating the efficacy and safety of different dosing regimens. Studies demonstrated that the twice-daily (BID) regimen of canagliflozin in combination with metformin was as effective as the once-daily (QD) regimen[2].
• Safety Profile: The combination therapy has been associated with some adverse effects, such as hypotension and decreases in eGFR, particularly in vulnerable patient populations. However, these effects are generally manageable with appropriate caution and monitoring[5].

Financial Performance and Revenue Growth

The financial performance of canagliflozin and its combination with metformin has been impressive.

• Revenue Growth: The sales of canagliflozin have grown significantly from $8 million in 2014 to $129 million in 2021. The combination therapy has contributed substantially to this growth, making it one of the key revenue drivers for the pharmaceutical companies involved[1].
• Market Share: The combination of canagliflozin and metformin has helped in maintaining and expanding market share in the competitive antidiabetic drug market. This is evident from the strong operational revenue and adjusted operational earnings growth reported by companies like Johnson & Johnson, which has a significant stake in this market[3].

Competitive Landscape

The antidiabetic drug market is highly competitive, with several new-generation drugs vying for market share.

• Competitive Advantage: The combination of canagliflozin and metformin offers a competitive advantage due to its proven efficacy, safety profile, and the convenience of a single tablet. This has helped in differentiating it from other antidiabetic medications[4].
• Market Positioning: The strategic positioning of this combination therapy has allowed it to capture a significant share of the market, particularly among patients who require more aggressive glycemic control.

Future Outlook

The future outlook for canagliflozin and metformin hydrochloride combination therapy looks promising.

• Continued Growth: With the increasing prevalence of type 2 diabetes and the ongoing need for effective and well-tolerated treatments, the sales of this combination therapy are expected to continue growing.
• New Indications: Potential new indications and line extensions could further expand the market reach and revenue potential of this combination.

Key Takeaways

• Effective Combination Therapy: The combination of canagliflozin and metformin has proven to be highly effective in achieving better glycemic control and weight reduction.
• Strong Financial Performance: The sales of canagliflozin and its combination with metformin have shown robust growth, contributing significantly to the revenue of pharmaceutical companies.
• Competitive Advantage: The combination therapy offers a competitive advantage due to its efficacy, safety, and convenience.
• Future Growth Potential: The market for this combination therapy is expected to continue growing, driven by the increasing need for effective diabetes treatments.

FAQs

What is the primary benefit of combining canagliflozin with metformin?

The primary benefit is the significant reduction in A1C levels and additional weight reduction, making it a more effective treatment option for type 2 diabetes.

How has the sales performance of canagliflozin been since its introduction?

Canagliflozin has shown steady growth in sales, from $0 million in 2012 to $129 million in 2021, with the combination therapy being a key driver of this growth.

What are the potential adverse effects of the canagliflozin and metformin combination?

Potential adverse effects include hypotension and decreases in eGFR, particularly in vulnerable patient populations such as those with cardiovascular disease or elderly patients.

How does the combination of canagliflozin and metformin compare to monotherapy with either drug?

The combination therapy has been shown to be more effective in reducing A1C levels and weight compared to monotherapy with either canagliflozin or metformin alone.

What is the regulatory status of the canagliflozin and metformin combination therapy?

The FDA has approved the fixed-dose combination of canagliflozin and metformin after evaluating its efficacy and safety through various clinical trials and pharmacokinetic studies.

Sources

1. Market Intelligence Report: Antidiabetic Drugs, 2012-2021. Canada.ca.
2. 204353Orig1s000 - accessdata.fda.gov. FDA.
3. 2019 - Annual Reports. AnnualReports.co.uk.
4. New Data Show Initial Use of Canagliflozin in Combination with Metformin Extended Release Significantly Improves A1C Levels in Adults with Type 2 Diabetes. PR Newswire.
5. Vokanamet, INN-canagliflozin metformin. EMA.europa.eu.