1. Product Overview & Specifications

Key Parameters

Unique Advantages: Macitentan demonstrates insurmountable antagonism (64% vs. 0% for bosentan/ambrisentan) due to slow receptor dissociation kinetics, enhancing therapeutic efficacy in pulmonary arterial smooth muscle cells.

2. Clinical Applications

Primary Indication

Macitentan is indicated for pulmonary arterial hypertension (PAH, WHO Group 1) to:

• Delay disease progression (e.g., mortality, clinical worsening)
• Reduce hospitalization rates
• Improve 6-minute walk distance (6MWD)

Mechanism of Action

As an endothelin receptor antagonist (ERA), Macitentan:

• Blocks ETA and ETB receptors, inhibiting vasoconstriction and vascular remodeling
• Reduces fibroblast proliferation and collagen deposition
• Shows non-competitive binding with prolonged receptor occupancy

3. Usage Guidelines

Dosage & Administration

• Standard Dose: 10 mg orally once daily
• Missed Dose: Take immediately if remembered; skip if near next dose
• Contraindications: Pregnancy (Boxed Warning), hypersensitivity to sulfonamides

Drug Interactions

4. Case Studies

SERAPHIN Trial (N=742)

Results: Macitentan 10 mg reduced risk of morbidity/mortality by 45% vs placebo (p<0.001) over 3.5 years. 6MWD improved by 12 meters (p=0.008).

Combination Therapy Study

Macitentan + tadalafil showed 56% reduction in clinical worsening vs monotherapy (HR 0.44, 95% CI 0.29–0.68).

5. Client Success Stories

Case 1: Idiopathic PAH Management

Patient: 48-year-old female, WHO FC III
Outcome: Sustained 6MWD improvement (320m → 410m) over 24 months; no hospitalization events.

Case 2: CTD-Associated PAH

Patient: 62-year-old male with scleroderma
Outcome: Delayed progression to FC IV by 18 months; maintained mean pulmonary artery pressure <35 mmHg.

6. Contact for Inquiries

For pricing, samples, or clinical data:
Email: info@vivalr.com
Tel: (86) 15866781826