ACVR2A (ActRIIA) Drug Discovery Landscape & Assay Solutions

Market Intelligence, Clinical Progress, and High-Purity Reagents for PAH, Muscle Atrophy, Obesity, and Oncology.

Target Overview

ACVR2A (Activin A receptor type IIA, UniProt P27037) is a transmembrane serine/threonine kinase receptor of the TGF-β superfamily. It contains a protein kinase domain and mediates signaling of activins, myostatin, and GDF11. Key naturally occurring mutations include rs34917571, rs764255410 (found in gastric adenocarcinoma), and a somatic mutation in clear cell renal carcinoma (VAR_064692). These variants provide important tools for studying functional alterations in disease.

TarMart Solution Ecosystem & Related Targets

Comprehensive reagent toolkit for ACVR2A drug discovery.

Component / Network Product Description Product Link
Antigen ACVR2A ECD-Fc Fusion Protein. High purity (>95%), Endotoxin <1 EU/μg. Sequence Verified. HEK293 Expressed (Native Glycosylation). View ACVR2A Products
Antigen (Mutant) ACVR2A mutant proteins (e.g., rs34917571) for variant-specific studies. View ACVR2A Products
Gene Delivery ACVR2A Promise-ORF / Lentivirus. Full-length ORF for stable cell lines. Preserves conformational epitopes. View ACVR2A Products
Benchmark Ab Anti-ACVR2A Biosimilars (Sotatercept and Bimagrumab sequence references). Recombinant positive controls for ligand-trap and mAb assays. View ACVR2A Products
Validator ACVR2A siRNA Set. For knockdown verification and specificity controls. View ACVR2A Products
Related Target A ACVR2B (ActRIIB). High homology (>70% ECD similarity); critical for selectivity counter-screening. View ACVR2B Products
Related Target B MSTN (Myostatin) / GDF8. Primary ligand for muscle wasting and metabolic pathways. View MSTN Products
Related Target C ACVR1B (ALK4) / ACVR1 (ALK2). Type I co-receptors for activin/BMP signaling. View ACVR1B Products
Critical Assay Challenge The TarMart Advantage (Technical Spec)
Ligand selectivity & cross-reactivity (Activin A, Myostatin, GDF11, BMP9) HEK293-expressed ACVR2A ECD-Fc with native glycosylation; multi-ligand binding kinetics via SPR/BLI.
Receptor isoform selectivity (ACVR2A vs ACVR2B) Matched pair of ACVR2A and ACVR2B ECD proteins; strictly verified by mass spec (>95% purity).
Cross-species evaluation (human, cyno, mouse) Ortholog proteins with sequence-verified glycosylation patterns; available for all three species.
Lack of positive controls for ligand-trap and mAb assays Clinical benchmark biosimilars (Sotatercept class, Bimagrumab class) included.
False positives in cell-based assays Validated ACVR2A siRNA and non-targeting controls for specificity checks, SMAD pathway verification.
High-concentration formulation stability High-purity ECD protein for DSF/SLS aggregation studies.

Live ACVR2A R&D Tracker

Market data changes daily. Access the latest global pipeline status directly:

Global Clinical Landscape & Future Outlook

The ACVR2A therapeutic field has entered a commercial validation phase following the FDA approval of sotatercept (Winrevair) for pulmonary arterial hypertension (PAH). Major players are now expanding into metabolic diseases: combination of ACVR2A/ACVR2B inhibitors (e.g., bimagrumab) with GLP-1 receptor agonists is emerging as a leading strategy to preserve muscle mass during weight loss. Meanwhile, next-generation Fc-fusions with refined selectivity profiles, bispecific antibodies targeting multiple TGF-β ligands, and high-concentration subcutaneous formulations are in active development. Additional frontiers include oncology (cachexia, solid tumors) and fibrosis. The field is shifting from first-generation ligand traps to more selective modalities that fine-tune receptor signaling to avoid vascular and reproductive side effects.

Competitive Modality & Indication Snapshot

Modality Representative Players Key Indications Critical Assay Need (Why TarMart?)
Fc-Fusion (Ligand Trap) Merck (Acceleron), Keros Therapeutics PAH, MDS/MPN Anemia Multi-ligand binding kinetics; need high-purity ECD-Fc (>95%)
Monoclonal Antibody Eli Lilly (Versanis), Novartis, Regeneron Obesity, Sarcopenia, Cancer Cachexia Isoform selectivity (ACVR2A vs ACVR2B); need homolog panel proteins
Bispecific / Multi-specific Scholar Rock, Biogen Cancer Cachexia, Fibrosis Heterodimer validation; need cross-reactive Abs vs ACVR2A/ACVR2B
Small Molecule Kinase Inhibitor Various Biotechs Oncology, Fibrosis Selectivity against related kinases; need purified kinase domain
Peptide Antagonists Multiple Biotechs Metabolic Disease Affinity maturation; need high-quality ECD for SPR/BLI