Macitentan - Generic Drug Details

What are the generic drug sources for macitentan and what is the scope of patent protection?

Macitentan is the generic ingredient in three branded drugs marketed by Alembic, Apotex, Aurobindo Pharma Ltd, Laurus, MSN, Mylan, Seasons Biotech, Sun Pharm, Torrent, Zydus Lifesciences, and Actelion, and is included in twelve NDAs. There are five patents protecting this compound and one Paragraph IV challenge. Additional information is available in the individual branded drug profile pages.

Macitentan has one hundred and one patent family members in thirty-five countries.

There are ten drug master file entries for macitentan. Twelve suppliers are listed for this compound. There is one tentative approval for this compound.

Summary for macitentan

International Patents:	101
US Patents:	5
Tradenames:	3
Applicants:	11
NDAs:	12
Drug Master File Entries:	10
Finished Product Suppliers / Packagers:	12
Raw Ingredient (Bulk) Api Vendors:	75
Clinical Trials:	61
Patent Applications:	1,274
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for macitentan
What excipients (inactive ingredients) are in macitentan?	macitentan excipients list
DailyMed Link:	macitentan at DailyMed

Recent Clinical Trials for macitentan

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

Sponsor	Phase
Gachon University Gil Medical Center	PHASE4
China-Japan Friendship Hospital	EARLY_PHASE1
Humanis Saglık Anonim Sirketi	PHASE1

See all macitentan clinical trials

Generic filers with tentative approvals for MACITENTAN

Applicant	Application No.	Strength	Dosage Form
		10MG	TABLET;ORAL

The 'tentative' approval signifies that the product meets all FDA standards for marketing, and, but for the patents / regulatory protections, it would approved.

Pharmacology for macitentan

Drug Class	Endothelin Receptor Antagonist
Mechanism of Action	Endothelin Receptor Antagonists

Anatomical Therapeutic Chemical (ATC) Classes for macitentan

C02KX	Antihypertensives for pulmonary arterial hypertension
C02K	OTHER ANTIHYPERTENSIVES
C02	ANTIHYPERTENSIVES
C	Cardiovascular system

Paragraph IV (Patent) Challenges for MACITENTAN

Tradename	Dosage	Ingredient	Strength	NDA	ANDAs Submitted	Submissiondate
OPSUMIT	Tablets	macitentan	10 mg	204410	11	2017-10-18

US Patents and Regulatory Information for macitentan

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Exclusivity Expiration
Actelion	OPSUMIT	macitentan	TABLET;ORAL	204410-001	Oct 18, 2013	AB	RX	Yes	Yes
Actelion	OPSYNVI	macitentan; tadalafil	TABLET;ORAL	218490-001	Mar 22, 2024		RX	Yes	No	7,094,781*PED				Y
Actelion	OPSYNVI	macitentan; tadalafil	TABLET;ORAL	218490-001	Mar 22, 2024		RX	Yes	No
Actelion	OPSYNVI	macitentan; tadalafil	TABLET;ORAL	218490-002	Mar 22, 2024		RX	Yes	Yes	8,268,847*PED				Y
Actelion	OPSUMIT	macitentan	TABLET;ORAL	204410-001	Oct 18, 2013	AB	RX	Yes	Yes	8,268,847*PED				Y
Torrent	MACITENTAN	macitentan	TABLET;ORAL	211107-001	Aug 5, 2024	AB	RX	No	No

EU/EMA Drug Approvals for macitentan

Company	Drugname	Inn	Product Number / Indication	Status	Generic	Biosimilar	Orphan	Marketing Authorisation	Marketing Refusal
Janssen-Cilag International N.V.	Opsumit	macitentan	EMEA/H/C/002697Opsumit, as monotherapy or in combination, is indicated for the long-term treatment of pulmonary arterial hypertension (PAH) in adult patients of WHO Functional Class (FC) II to III.Efficacy has been shown in a PAH population including idiopathic and heritable PAH, PAH associated with connective tissue disorders, and PAH associated with corrected simple congenital heart disease.	Authorised	no	no	yes	2013-12-20

International Patents for macitentan

Country	Patent Number	Title	Estimated Expiration
Australia	2006290309
Brazil	PI0615898
Canada	2621273
China	101262847
Cyprus	1113395
Denmark	1928409

Supplementary Protection Certificates for macitentan

Patent Number	Supplementary Protection Certificate	SPC Country	SPC Expiration	SPC Description
2059246	PA2024537	Lithuania		PRODUCT NAME: (A) MACITENTANO ARBA JO FARMACINIU POZIURIU PRIIMTINOS DRUSKOS IR (B)TADALAFILIO ARBA JO FARMACINIU POZIURIU PRIIMTINOS DRUSKOS DERINYS; REGISTRATION NO/DATE: EU/1/24/1859 20240927
2059246	LUC00371	Luxembourg		PRODUCT NAME: A COMBINATION OF (A) MACITENTAN OR A PHARMACEUTICALLY ACCEPTABLE SALT THEREOF AND (B) TADALAFIL OR A PHARMACEUTICALLY ACCEPTABLE SALT THEREOF; AUTHORISATION NUMBER AND DATE: EU/1/24/1859 20240930
2059246	2024C/552	Belgium		PRODUCT NAME: EEN COMBINATIE VAN (A) MACITENTAN OF EEN FARMACEUTISCH AANVAARDBAAR ZOUT HIERVAN EN (B) TADALAFIL OF EEN FARMACEUTISCH AANVAARDBAAR ZOUT HIERVAN; AUTHORISATION NUMBER AND DATE: EU/1/24/1859 20240930
2059246	24C1054	France		PRODUCT NAME: COMBINAISON DE (A) MACITENTAN OU L'UN DE SES SELS PHARMACEUTIQUEMENT ACCEPTABLES ET (B) TADALAFIL OU L'UN DE SES SELS PHARMACEUTIQUEMENT ACCEPTABLES; REGISTRATION NO/DATE: EU/1/24/1859 20240930
1345920	CR 2014 00012	Denmark		PRODUCT NAME: MACITENTAN OG FARMACEUTISK ACCEPTABLE SALTE HERAF; REG. NO/DATE: EU/1/13/893 20131227
1345920	122014000056	Germany		PRODUCT NAME: MACITENTAN; REGISTRATION NO/DATE: EU/1/13/893/001-003 20131220

Macitentan Market Dynamics and Financial Trajectory (US and Global) Macitentan, an endothelin receptor antagonist marketed for pulmonary arterial hypertension (PAH), has transitioned from early growth to a more mature, competitive market. Forecastable revenue is driven by guideline-directed adoption, PAH patient persistence, payer mix, and loss-of-exclusivity timelines for branded supply. The financial trajectory is also shaped by biosimilar or generic entry risk at the drug-label level (via generic macitentan tablets) and by patient-level uptake shifts toward competing oral PAH agents.

What is macitentan and what are its main revenue drivers?

Macitentan (Opsumit, active ingredient macitentan) is used for PAH to reduce the risk of disease progression and improve exercise capacity. Revenue drivers are typically less about dose escalation and more about sustained patient coverage and formulary positioning.

Primary revenue drivers

Last updated: June 20, 2026

• PAH prevalence and treatment penetration: number of diagnosed PAH patients treated with oral PAH therapies.
• Persistence and switching: continued macitentan use vs switching to other PAH combinations.
• Formulary status and rebates: payer-specific access, net price, and tender dynamics.
• Competition in the oral PAH class: adoption of alternative endothelin receptor antagonists, prostacyclin pathway agents, and soluble guanylate cyclase stimulators.
• Exclusivity and entry risk: generic or authorized generic impact after patent cliff.

Key market characteristic

• PAH is chronic, but the market is fragmented by severity and combination strategy, which limits simple “dose-volume” growth and makes payer access and persistence critical.

Which dosing and label scope matter commercially?

Macitentan is commercialized as an oral tablet. Commercial outcomes depend on:

• regimen selection in newly diagnosed vs stable patients
• combination use patterns (common in PAH)
• clinician choice under guideline recommendations

How do combination regimens affect macitentan revenue?

In PAH, macitentan revenue is influenced by combination uptake more than monotherapy. Net revenue sensitivity rises when:

• payers require step therapy or prefer cheaper generics in combination
• competitors offer superior tolerability or dosing convenience profiles
• real-world titration practices change due to safety signals or tolerability comparisons

How has macitentan’s market share evolved versus other PAH drugs?

Macitentan competes across multiple PAH pillars: endothelin receptor antagonists (ERAs), PDE5 inhibitors, soluble guanylate cyclase stimulators (sGCs), and prostacyclin pathway agents. Market share evolution is driven by both clinical positioning and economics of access.

Competitive dynamics that typically shift share

• Net price pressure as branded competitors broaden discounting.
• Therapeutic sequencing: many payers and clinicians favor combinations that minimize hospitalization risk.
• Real-world tolerability: anemia, hepatic monitoring burden, and edema can influence persistence.
• Concentration of specialists: PAH centers drive prescribing and are sensitive to formulary restrictions.

Which PAH drug categories most affect macitentan uptake?

• Other oral ERAs (class substitution)
• Oral sGC stimulators (e.g., riociguat)
• Oral prostacyclin pathway approaches (e.g., selexipag)
• PDE5 inhibitors used in background regimens

How does class substitution change pricing power?

Once generics or authorized generics enter the ERA segment, macitentan’s pricing power can fall quickly even when clinical preference persists. The result is usually:

• reduced net price after rebate renegotiation
• more aggressive payer steering toward lower-cost options
• higher loss-of-revenue risk on stable patient pools

When do generic entry risks for macitentan accelerate, and what does that do to revenue?

Branded macitentan revenue risk peaks when exclusivity and enforceable patent barriers decline for macitentan tablets in key markets. Generic entry commonly creates a steep first-year price compression with slower volume rebound.

Generic entry impact pattern

• Year of first generic launch: largest net price decline (often steep in private-insurance and tender-driven markets).
• Post-launch years: volume share consolidates among the lowest-cost suppliers, and rebate structures reconfigure.

What matters for entry timing in US and EU?

Macitentan’s entry timing is determined by:

• patent expiry and litigation outcomes
• Orange Book-listed patents (for listed drug macitentan tablet products)
• paragraph IV and settlement agreements (if any)
• national regulatory and pricing policies

No Orange Book expiration, paragraph IV filing, or settlement dates are provided in the current prompt, so a precise timeline cannot be stated here.

What is the financial trajectory for macitentan (growth, maturity, and drawdowns)?

Macitentan’s financial trajectory typically follows a lifecycle pattern:

1. Launch and uptake: formulary adoption in major PAH centers; steady prescription ramp.
2. Maturity: plateau as PAH treated population growth slows relative to competitors’ penetration.
3. Drawdown: revenue compression as payer access shifts, discounted branded dynamics intensify, and generic entry approaches.

What to track for the trajectory

• US net sales vs international: international markets often capture earlier share if patent protection differs or if uptake lags.
• Prescription trend: pharmacy claims often show earlier effects than revenue because rebates and gross-to-net change later.
• Patient persistence: retention in stable patients supports maintenance revenue until substitution or combination changes.
• Channel mix: PAH drugs often show different dynamics between specialty pharmacy and hospital outpatient acquisition.

Which P&L line items most reflect market dynamics?

• Gross-to-net (rebates and discounts) is usually the fastest-moving lever.
• Returns and chargebacks rise after payer policy changes or tender switches.
• R&D is usually stable after initial product maturation, so margin sensitivity is mostly commercial.

How do payer dynamics and reimbursement shape macitentan’s net sales?

Payer mix and formulary access are decisive for PAH drugs because they are specialty, chronic, and expensive relative to many alternative therapies.

Key payer levers

• Formulary tiers and prior authorization: can delay uptake and reduce persistence.
• Specialty pharmacy contracting: impacts acquisition cost and throughput.
• Reference pricing and therapeutic substitution: particularly important when generics enter the ERA market.
• Patient assistance programs: often stabilize short-term access but do not prevent long-term payer steering.

What is the likely effect of rebate renegotiations as competition increases?

As competitor discounting and generic pressure rise:

• branded net price drops
• volume remains supported short-term by physician preference
• net sales flatten even if prescriptions remain stable
• revenue sensitivity increases around tender cycles and formulary updates

How does competition in PAH impact macitentan profitability and margins?

Macitentan profitability depends on how quickly pricing pressure hits net sales and whether cost of goods scales with demand.

Margin drivers

• lower net price vs stable manufacturing costs
• incremental commercial spend needed to defend access
• costs tied to pharmacovigilance and REMS-like program components (if applicable)

What delivery or formulation factors matter?

For oral PAH agents, formulation differences are usually secondary to:

• safety monitoring burden
• tolerability profile
• dosing schedule convenience These factors influence persistence and the likelihood of switching.

What regional factors change macitentan’s global sales trajectory?

Regional differences in:

• patent strength and timeline
• tender systems
• willingness to cover expensive biologically active branded therapies
• local generic adoption speed can drive divergence between US and EU/Asia sales.

Typical regional divergence mechanisms

• faster generic substitution where enforcement is weaker or where local approvals reduce friction
• slower decline in markets with strict reimbursement controls that delay substitution

How strong is the patent and regulatory barrier profile for macitentan?

This section requires patent listing data and regulatory status. The prompt does not provide Orange Book entries, expiration dates, or patent numbers, so a defensible patent strength assessment cannot be produced.

What market scenarios define macitentan’s next 3 to 5 years?

With macitentan in a mature therapeutic class and PAH pricing under sustained pressure, the scenarios usually hinge on:

• timing of generic or authorized generic entry in key markets
• payer shift toward lower-cost ERAs or preferred oral combinations
• persistence under real-world tolerability and monitoring patterns

Scenario framework (non-quantified)

• Base case: steady prescriptions but ongoing net price erosion; revenue declines gradually.
• Downside: faster payer substitution around competitive entrants or generic supply; sharper net price compression.
• Upside: stronger persistence and favorable formulary defense; delayed generic impact and more stable net price.

No quantified scenario bands are provided because required market and regulatory dates are not included in the prompt.

Key Takeaways

• Macitentan’s financial trajectory is governed by PAH treatment penetration, patient persistence, and payer access more than pure dose growth.
• Net sales are highly sensitive to rebate intensity and formulary steering as competitive PAH oral regimens intensify.
• The biggest revenue risk typically concentrates around the timing of generic/authorized-generic entry and enforceable patent barrier decline for macitentan tablets in major markets.
• Regional pricing and substitution speed can cause materially different trajectories across US vs non-US markets.
• A precise patent-tied exclusivity and revenue cliff analysis is not possible from the information provided in the prompt.

FAQs

1. How do macitentan rebates and patient assistance programs affect gross-to-net and reported revenue trends?
2. What competitive factors most influence macitentan persistence in stable PAH patients versus switching after safety events?
3. How do tender pricing and specialty pharmacy contracting differ for macitentan across EU countries?
4. What is the typical impact on macitentan net sales in the first year after generic entry in the US?
5. How does combination therapy selection by PAH centers shift macitentan share compared with other oral PAH agents?

References (APA)

1. (No citable sources were provided in the prompt.)