ETRASIMOD ARGININE - Generic Drug Details

What are the generic drug sources for etrasimod arginine and what is the scope of freedom to operate?

Etrasimod arginine is the generic ingredient in one branded drug marketed by Pfizer and is included in one NDA. There are seven patents protecting this compound. Additional information is available in the individual branded drug profile pages.

Etrasimod arginine has ninety-eight patent family members in twenty-seven countries.

Two suppliers are listed for this compound.

Summary for ETRASIMOD ARGININE

International Patents:	98
US Patents:	7
Tradenames:	1
Applicants:	1
NDAs:	1
Finished Product Suppliers / Packagers:	2
DailyMed Link:	ETRASIMOD ARGININE at DailyMed

DrugPatentWatch^® Estimated Loss of Exclusivity (LOE) Date for ETRASIMOD ARGININE

Constraining patent/regulatory exclusivity:

NEW CHEMICAL ENTITY

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 ETRASIMOD ARGININE

Drug Class	Sphingosine 1-phosphate Receptor Modulator
Mechanism of Action	Sphingosine 1-Phosphate Receptor Modulators

Anatomical Therapeutic Chemical (ATC) Classes for ETRASIMOD ARGININE

L04AE	Sphingosine-1-phosphate (S1P) receptor modulators
L04A	IMMUNOSUPPRESSANTS
L04	IMMUNOSUPPRESSANTS
L	Antineoplastic and immunomodulating agents

US Patents and Regulatory Information for ETRASIMOD ARGININE

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Exclusivity Expiration
Pfizer	VELSIPITY	etrasimod arginine	TABLET;ORAL	216956-001	Oct 12, 2023		RX	Yes	Yes	9,126,932
Pfizer	VELSIPITY	etrasimod arginine	TABLET;ORAL	216956-001	Oct 12, 2023		RX	Yes	Yes	11,091,435		Y	Y
Pfizer	VELSIPITY	etrasimod arginine	TABLET;ORAL	216956-001	Oct 12, 2023		RX	Yes	Yes	11,884,626
Pfizer	VELSIPITY	etrasimod arginine	TABLET;ORAL	216956-001	Oct 12, 2023		RX	Yes	Yes	8,580,841		Y	Y
Pfizer	VELSIPITY	etrasimod arginine	TABLET;ORAL	216956-001	Oct 12, 2023		RX	Yes	Yes	10,676,435
Pfizer	VELSIPITY	etrasimod arginine	TABLET;ORAL	216956-001	Oct 12, 2023		RX	Yes	Yes	10,301,262		Y	Y
Pfizer	VELSIPITY	etrasimod arginine	TABLET;ORAL	216956-001	Oct 12, 2023		RX	Yes	Yes

International Patents for ETRASIMOD ARGININE

Country	Patent Number	Title	Estimated Expiration
Japan	2011529049
European Patent Office	3310760	SEL L-ARGININE CRISTALLIN D'ACIDE (R)-2-(7-(4-CYCLOPENTYL-3-(TRIFLUOROMÉTHYL)BENZYLOXY)-1,2,3,4-TÉTRAHYDROCYCLO-PENTA[B]INDOL-3-YL)ACÉTIQUE (COMPOSÉ 1) POUR UNE UTILISATION DANS DES TROUBLES ASSOCIÉS AU RÉCEPTEUR DE S1P1 (CRYSTALLINE L-ARGININE SALT OF (R)-2-(7-(4-CYCLOPENTYL-3-(TRIFLUOROMETHYL)BENZYLOXY)-1,2,3,4-TETRAHYDROCYCLO-PENTA[B]INDOL-3-YL)ACETIC ACID(COMPOUND1) FOR USE IN SIPI RECEPTOR-ASSOCIATED DISORDERS)
South Korea	102595163
China	116850181	治疗与S1P1受体有关的病症的方法 (Methods of treating conditions associated with s1p1 receptor)
Israel	285890
Mexico	2011000879	DERIVADOS DE ÁCIDO 1,2,3,4-TETRAHIDROCICLOPENTA [B] INDOL-3-IL) ACETICO SUSTITUIDOS ÚTILES EN EL TRATAMIENTO DE ENFERMEDADES AUTOINMUNE E INFLAMATORIAS. (SUBSTITUTED 1,2,3,4- TETRAHYDROCYCLOPENTA[b]INDOL-3-YL) ACETIC ACID DERIVATIVES USEFUL IN THE TREATMENT OF AUTOIMMUNE AND INFLAMMATORY DISORDERS.)
Japan	6895378

ETRASIMOD ARGININE Market Analysis and Financial Projection Experimental

Market Dynamics and Financial Trajectory for Etrasimod Arginine

Introduction to Etrasimod Arginine

Etrasimod arginine, developed by Arena Pharmaceuticals and now under Pfizer, is an oral, once-daily, selective sphingosine 1-phosphate (S1P) receptor modulator. It is primarily being investigated for the treatment of moderately to severely active ulcerative colitis (UC), along with other immuno-inflammatory diseases such as Crohn’s Disease, atopic dermatitis, eosinophilic esophagitis, and alopecia areata[2][4].

Clinical Efficacy and Safety Profile

The clinical efficacy of etrasimod arginine has been demonstrated through several Phase 3 trials, including the ELEVATE UC 12 and ELEVATE UC 52 studies. These trials showed statistically significant improvements in clinical remission, endoscopic improvement, symptomatic remission, and mucosal healing compared to placebo. For instance, in the ELEVATE UC 52 trial, 27.0% of patients on etrasimod achieved clinical remission at week 12, compared to 7.4% on placebo, with sustained benefits observed at week 52[1][4].

The safety profile of etrasimod arginine has been consistent with previous studies, with common adverse events including headache, worsening of UC, COVID-19 infection, dizziness, pyrexia, arthralgia, abdominal pain, and nausea. Notably, there were no reports of bradycardia or atrioventricular block as serious adverse events[1][4].

Regulatory Status and Approval Timeline

The FDA and EMA have accepted the regulatory submissions for etrasimod arginine. The FDA's decision is expected in the second half of 2023, while the EMA's decision is anticipated in the first half of 2024. These regulatory milestones are crucial for the drug's market entry and subsequent financial performance[1].

Market Potential and Competitive Landscape

The market for ulcerative colitis treatments is significant and growing, driven by the increasing prevalence of the disease and the need for effective oral therapies. Etrasimod arginine, if approved, will enter a competitive market that includes biologics and JAK inhibitors. However, its oral administration and favorable safety profile could position it as a preferred option for patients who have failed or are intolerant to conventional or advanced therapies[4].

Pharmacokinetics and Patient Compliance

Etrasimod arginine has a favorable pharmacokinetic profile, with peak plasma concentrations attained approximately 4 hours after oral administration and steady-state concentrations achieved in about 7 days. The drug's bioavailability is dose-proportional, and its absorption is not affected by food intake. This profile supports once-daily dosing, which can enhance patient compliance[3].

Patent Protection and Generic Competition

The patent protection for etrasimod arginine extends until June 21, 2036, for several key patents, ensuring a significant period of market exclusivity. This protection is crucial for Pfizer to recoup its investment in the drug's development and to generate substantial revenue before generic competition emerges[5].

Financial Projections and Revenue Potential

Given the positive clinical trial results and the anticipated regulatory approvals, etrasimod arginine is expected to generate significant revenue for Pfizer. The drug's potential to address a substantial unmet need in the treatment of ulcerative colitis, combined with its oral administration and favorable safety profile, positions it for strong market uptake.

Impact of COVID-19 and Global Economic Factors

The COVID-19 pandemic has introduced uncertainties in the pharmaceutical industry, affecting clinical trial timelines, regulatory submissions, and market dynamics. However, Pfizer's robust financial position and diversified portfolio are expected to mitigate these risks. Global economic factors, such as healthcare spending trends and reimbursement policies, will also influence the drug's financial trajectory[1][4].

Expert Insights and Market Analysis

"Etrasimod, if approved, could be a potential breakthrough option for patients with ulcerative colitis who aren’t able to experience improvement on current therapies," said Michael Corbo, Chief Development Officer, Inflammation & Immunology, Pfizer Global Product Development. This sentiment reflects the optimism among industry experts regarding the drug's market potential[4].

Key Takeaways

• Clinical Efficacy: Etrasimod arginine has shown significant clinical remission and safety benefits in Phase 3 trials.
• Regulatory Status: FDA and EMA approvals are anticipated in 2023 and 2024, respectively.
• Market Potential: The drug is poised to enter a competitive but growing market for UC treatments.
• Pharmacokinetics: Favorable pharmacokinetic profile supports once-daily dosing and patient compliance.
• Patent Protection: Extensive patent protection until 2036 ensures market exclusivity.
• Financial Projections: Significant revenue potential driven by strong market uptake and unmet medical need.

FAQs

Q1: What is etrasimod arginine used for? Etrasimod arginine is primarily used for the treatment of moderately to severely active ulcerative colitis (UC) and is being investigated for other immuno-inflammatory diseases.

Q2: What are the key clinical trial results for etrasimod arginine? Clinical trials, such as ELEVATE UC 12 and ELEVATE UC 52, have shown statistically significant improvements in clinical remission, endoscopic improvement, and other key endpoints compared to placebo.

Q3: When are the regulatory approvals expected? The FDA's decision is expected in the second half of 2023, and the EMA's decision is anticipated in the first half of 2024.

Q4: What is the safety profile of etrasimod arginine? The safety profile is consistent with previous studies, with common adverse events including headache, worsening of UC, and others, but no reports of serious cardiac issues.

Q5: How long is the patent protection for etrasimod arginine? The patent protection for etrasimod arginine extends until June 21, 2036.

Cited Sources

1. Pfizer Announces FDA and EMA Acceptance of Etrasimod Regulatory Submissions for Ulcerative Colitis - Pfizer Press Release.
2. Arena Pharmaceuticals, Inc. - Drug pipelines, Patents, Clinical trials - Synapse.
3. Etrasimod Arginine Monograph for Professionals - Drugs.com.
4. Pfizer Announces Positive Top-Line Results for Phase 3 Trial of Etrasimod in Ulcerative Colitis Patients - Pfizer Press Release.
5. Drug Patents containing Etrasimod Arginine - Pharsight.