pharmacopeia
GET
/api/v1/drug/sotatercept

Mechanism of action

Sourced from openFDA

Sotatercept-csrk, a recombinant activin receptor type IIA-Fc (ActRIIA-Fc) fusion protein, is an activin signaling inhibitor that binds to activin A and other TGF- β superfamily ligands. As a result, sotatercept-csrk improves the balance between the pro-proliferative (ActRIIA/Smad2/3-mediated) and anti-proliferative (BMPRII/Smad1/5/8-mediated) signaling to modulate vascular proliferation.

Activin Signaling

Indications

Sourced from openFDA
  • WINREVAIR™ is indicated for the treatment of adults with pulmonary arterial hypertension (PAH, Group 1 pulmonary hypertension) to improve exercise capacity and World Health Organization (WHO) functional class (FC), and reduce the risk of clinical worsening events including hospitalization for PAH, lung transplantation and death [see Clinical Studies (14.1) ] . WINREVAIR is an activin signaling inhibitor indicated for the treatment of adults with pulmonary arterial hypertension (PAH, WHO Group 1 pulmonary hypertension) to improve exercise capacity and WHO functional class (FC), and reduce the risk of clinical worsening events, including hospitalization for PAH, lung transplantation and death.ICD-10: I27.0

Contraindications

Sourced from openFDA
  • None.contraindicated

Dosage & administration

Sourced from openFDA

The recommended starting dose is 0.3 mg/kg by subcutaneous injection. ( 2.1 ) The recommended target dose is 0.7 mg/kg every 3 weeks by subcutaneous injection. ( 2.2 ) Dosage modifications due to increased hemoglobin (Hgb) and decreased platelets may be necessary. Check Hgb and platelets before each dose for the first 5 doses, or longer if values are unstable, and monitor periodically thereafter. ( 2.3 ) See full prescribing information for preparation and administration instructions. ( 2.4 ) 2.1 Recommended Starting Dosage WINREVAIR is administered once every 3 weeks by subcutaneous injection according to patient body weight. The starting dose of WINREVAIR is 0.3 mg/kg. Obtain hemoglobin (Hgb) and platelet count prior to the first dose of WINREVAIR. Do not initiate treatment if platelet count is <50,000/mm 3 (<50 x 10 9 /L) [see Dosage and Administration (2.3) ] . Injection volume for starting dose is calculated based on patient weight as follows: Injection Volume (mL) = Weight (kg) x 0.3 mg/kg 50 mg/mL Injection volume should be rounded to the nearest 0.1 mL. For example: (70 kg x 0.3 mg/kg) ÷ 50 mg/mL = 0.42 mL, rounds to 0.4 mL See Table 1 for selecting the appropriate kit based on calculated injection volume for starting dose. Table 1: Kit Type Based on Injection Volume for Dose of 0.3 mg/kg Injection Volume (mL) Kit Type 0.2 to 0.9 45 mg kit (containing 1 x 45 mg vial) 1 to 1.1 60 mg kit (containing 1 x 60 mg vial) 2.2 Recommended Target Dosage After verifying acceptable Hgb and platelet count, increase to the target dose of 0.7 mg/kg.

Warnings & precautions

Sourced from openFDA

Erythrocytosis: If severe, may increase the risk of thromboembolic events and hyperviscosity syndrome. Monitor Hgb before each dose for the first 5 doses, or longer if values are unstable, and periodically thereafter to determine if dose adjustments are required. ( 5.1 ) Severe Thrombocytopenia: May increase the risk of bleeding. Monitor platelets before each dose for the first 5 doses, or longer if values are unstable, and periodically thereafter to determine if dose adjustments are required. ( 5.2 ) Serious Bleeding: Serious bleeding events were reported and were more likely with concomitant prostacyclin and/or antithrombotic agents, or with low platelet counts. Do not administer WINREVAIR if the patient is experiencing serious bleeding. ( 5.3 ) Embryo-Fetal Toxicity: May cause fetal harm. Advise females of reproductive potential of the potential risk to a fetus and use of effective contraception. ( 5.4 , 8.1 , 8.3 ) Impaired Fertility: May impair female and male fertility. ( 5.5 , 8.3 , 13.1 ) 5.1 Erythrocytosis WINREVAIR may increase hemoglobin. Severe erythrocytosis may increase the risk of thromboembolic events or hyperviscosity syndrome. In clinical studies, moderate elevations in Hgb (>2 g/dL above ULN) occurred in 15% of patients taking WINREVAIR while no elevations ≥4 g/dL above ULN were observed. Monitor Hgb before each dose for the first 5 doses, or longer if values are unstable, and periodically thereafter, to determine if dose adjustments are required [see Dosage and Administration (2.3) , Adverse Reactions (6.1) ] .

Adverse reactions

Sourced from openFDA

The following clinically significant adverse reactions are described elsewhere in the labeling: Erythrocytosis [see Warnings and Precautions (5.1) ] Severe Thrombocytopenia [see Warnings and Precautions (5.2) ] Serious Bleeding [see Warnings and Precautions (5.3) ] Embryo-Fetal Toxicity [see Warnings and Precautions (5.4) ] Impaired Fertility [see Warnings and Precautions (5.5) ] The most common (≥10% in patients receiving WINREVAIR and 5% more than placebo) adverse reactions were infections, epistaxis, telangiectasia, diarrhea, headache, rash, increased hemoglobin, dizziness, erythema, and gingival bleeding. ( 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact Merck Sharp & Dohme LLC at 1-877-888-4231 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch 6.1 Clinical Trials Experience Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice. STELLAR The following data reflect exposure to WINREVAIR in the STELLAR trial. Adult PAH patients with WHO FC II or III (n=323) were randomized in a 1:1 ratio to receive WINREVAIR or placebo in combination with background standard of care therapies. Patients received a starting dose of 0.3 mg/kg via SC injection and the dose was increased to the target dose of 0.7 mg/kg administered once every 3 weeks for 24 weeks.

Use in specific populations

Sourced from openFDA

Lactation: Breastfeeding not recommended. ( 8.2 ) 8.1 Pregnancy Risk Summary Based on findings in animal reproduction studies, WINREVAIR may cause fetal harm when administered to a pregnant woman. There are risks to the mother and the fetus associated with pulmonary arterial hypertension in pregnancy (see Clinical Considerations ) . There are no available data on WINREVAIR use in pregnant women to inform a drug-associated risk of major birth defects, miscarriage, or adverse maternal or fetal outcomes. In animal reproduction studies, administration of WINREVAIR to pregnant rats and rabbits during the period of organogenesis resulted in adverse developmental outcomes, including embryo-fetal mortality, alterations to growth, and structural variations at exposures 4-fold and 0.6-fold (based on area under the curve [AUC]) above those occurring at the maximum recommended human dose (MRHD), respectively (see Data ) . Advise pregnant women of the potential risk to a fetus [see Use in Specific Populations (8.3) ] . The background risk of major birth defects and miscarriage for the indicated population is not known. All pregnancies have a background risk of birth defect, loss, or other adverse outcomes. In the U.S. general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies is 2% to 4% and 15% to 20%, respectively.

Pharmacokinetics

Sourced from openFDA
Metabolism
Following subcutaneous administration of 0.7 mg/kg WINREVAIR every three weeks to PAH patients (PULSAR, SPECTRA, and STELLAR), the steady state geometric mean (%CV) area under the time concentration curve (AUC) is 171.3 mcg×d/mL (34.2%), and peak concentration (C max ) is 9.7 mcg/mL (30%). Sotatercept-csrk AUC and C max increased proportionally with dose.

Overdosage

Sourced from openFDA

In healthy volunteers, WINREVAIR dosed at 1 mg/kg resulted in increases in Hgb associated with hypertension; both improved with phlebotomy. In the event of overdose, monitor closely for increases in Hgb and blood pressure, and provide supportive care as appropriate. WINREVAIR is not dialyzable.

Approval history

Sourced from openFDA
  • Mar 26, 2024BLABLA761363Merck Sharp Dohme

FAERS reports

View JSON
Reference statistics only. FAERS reports are voluntarily submitted and are not incidence rates, safety signals, or causal evidence. Counts reflect reporting volume — how often a reaction was reported, not how often it occurs. For decision-grade use, consult openFDA and the FAERS Public Dashboard directly.
3,905 total reports matchedLatest report Share = reports listing the reaction ÷ total matched reports. Rows can sum to >100% because a single report often lists multiple reactions.
  1. 1Headache52513%
  2. 2Diarrhoea40410%
  3. 3Dyspnoea40210%
  4. 4Epistaxis3428.8%
  5. 5Fatigue3258.3%
  6. 6Dizziness3128.0%
  7. 7Nausea3017.7%
  8. 8Haemoglobin Increased2105.4%
  9. 9Dyspnoea Exertional1744.5%
  10. 10Vomiting1604.1%
  11. 11Product Dose Omission Issue1503.8%
  12. 12Hypotension1473.8%
  13. 13Pain In Extremity1453.7%
  14. 14Pain1433.7%
  15. 15Pneumonia1423.6%

Clinical trials

View JSON

The 10 most recently updated of 40 ClinicalTrials.gov registrations naming Sotatercept as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

Frequently asked questions

How does Sotatercept work?
Sotatercept-csrk, a recombinant activin receptor type IIA-Fc (ActRIIA-Fc) fusion protein, is an activin signaling inhibitor that binds to activin A and other TGF- β superfamily ligands. As a result, sotatercept-csrk improves the balance between the pro-proliferative (ActRIIA/Smad2/3-mediated) and anti-proliferative (BMPRII/Smad1/5/8-mediated) signaling to modulate vascular proliferation.
What is Sotatercept used for?
According to FDA labeling, Sotatercept carries indications including: WINREVAIR™ is indicated for the treatment of adults with pulmonary arterial hypertension (PAH, Group 1 pulmonary hypertension) to improve exercise capacity and World Health Organization (WHO) functional class (FC), and reduce the risk of clinical worsening events including hospitalization for PAH, lung transplantation and death [see Clinical Studies (14.1) ] . WINREVAIR is an activin signaling inhibitor indicated for the treatment of adults with pulmonary arterial hypertension (PAH, WHO Group 1 pulmonary hypertension) to improve exercise capacity and WHO functional class (FC), and reduce the risk of clinical worsening events, including hospitalization for PAH, lung transplantation and death.. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.
What class of drug is Sotatercept?
Sotatercept is classified as Antihypertensives for pulmonary arterial hypertension, Activin Signaling Inhibitor, Activin Signaling Inhibitors, Cytokine Receptor Superfamily Interactions, Fusion Protein Interactions, Cellular Proliferation Alteration.
What are the brand names for Sotatercept?
Sotatercept is marketed under brand names including Winrevair.
What are the contraindications for Sotatercept?
Sotatercept labeling lists contraindications including: None.. Always consult the full prescribing information and a clinician.
Note. Data for sotatercept is illustrative MVP content compiled from public sources. pharmacopeia is for educational and informational use only and is not a substitute for professional medical advice.

Search pharmacopeia

Search drugs, classes, and ingredients