Market Intelligence, Clinical Progress, and High-Purity Reagents for Prostate Cancer and Resistance Mutation Development.
TarMart Solution Ecosystem & Related Targets
Comprehensive reagent toolkit for Androgen Receptor drug discovery. Select your modality below:
| Component / Network | Product Description | Product Link |
|---|---|---|
| Antigen | AR LBD, NTD & Mutant Recombinant Proteins High purity (>95%), Endotoxin <1EU/μg. Sequence Verified. Includes clinically relevant mutations: T878A, F876L, H875Y, W741L, L702H. |
View AR Products |
| Gene Delivery | AR / ORF Premade Lentivirus Full-length AR for stable cell line construction (LNCaP, MDA-MB-453). |
View AR Products |
| Benchmark Ab | Anti-AR Reference (Sequence of Enzalutamide binding domain) Recombinant positive control for competitive binding assays and IHC/WB standardization. |
View AR Products |
| Validator | AR siRNA Set For knockdown verification and specificity controls in cell-based assays. |
View AR Products |
| Related Target A | AR-V7 Constitutively active splice variant lacking LBD; critical resistance mechanism in mCRPC. |
View AR-V7 Products |
| Related Target B | CYP17A1 Upstream androgen biosynthesis enzyme; target of abiraterone for combination therapy. |
View CYP17A1 Products |
| Related Target C | PARP1 Synergistic target for HRR-mutated prostate cancer combinations (e.g., olaparib). |
View PARP1 Products |
| Related Target D | TMPRSS2 Androgen-regulated serine protease; downstream AR target gene and biomarker for PCa progression. |
View TMPRSS2 Products |
| Related Target E | FKBP5 AR co-chaperone regulating receptor stability and nuclear translocation. |
View FKBP5 Products |
| Critical Assay Challenge | The TarMart Advantage (Technical Spec) |
|---|---|
| Resistance Mutation Screening (F876L, T878A, W741L, H875Y, L702H) | Single-point mutant panels (HEK293 expressed, >95% purity, Mass Spec verified for precise mutation incorporation) |
| PROTAC Ternary Complex Validation | High-purity full-length AR (native folding) and E3 ligases (VHL/CRBN) for SPR/TR-FRET/AlphaScreen |
| Splice Variant Specificity (AR-V7) | Domain-specific truncated constructs (NTD-only) verified by mass spectrometry and Theoretical MW |
| Steroid Receptor Selectivity (vs GR, PR, MR) | Homolog panel proteins (GRα, PR-B, MR) with identical expression systems for orthogonal binding assays |
| Lack of Reliable Cell Models | Lentiviral particles for rapid generation of AR-dependent reporter cell lines and nuclear translocation assays |
| Nuclear Translocation Quantification | Lentivirus stable cell line construction with selectable markers; Endotoxin controlled (<100EU/mL) |
Live AR R&D Tracker
Market data changes daily. Access the latest global pipeline status directly:
Global Clinical Landscape & Future Outlook
The race for next-generation Androgen Receptor therapeutics is intensifying, with major players shifting focus from traditional competitive antagonists (enzalutamide, apalutamide) to PROteolysis TArgeting Chimeras (PROTACs) and N-Terminal Domain (NTD) inhibitors capable of bypassing acquired resistance driven by LBD point mutations (e.g., T878A, F876L, H875Y) and the constitutively active AR-V7 splice variant. As first-generation therapies reach peak clinical utility, approximately 60% of early-stage pipeline assets now employ novel mechanisms (degraders, allosteric modulators), with next-wave R&D targeting CNS-penetrant degraders, mutation-selective binders, and tissue-selective AR modulators (SARMs) for non-oncology indications. The climb to best-in-class status increasingly demands orthogonal assay platforms that distinguish wild-type vs. mutant AR, evaluate ternary complex formation, and quantify AR-V7-dependent transcription.
Competitive Modality & Indication Snapshot
| Modality | Representative Players | Key Indications | Critical Assay Need (Why TarMart?) |
|---|---|---|---|
| Small Molecule Antagonist (LBD) | Astellas/Pfizer (Enzalutamide), Janssen (Apalutamide), Bayer (Darolutamide) | Prostate Cancer (mCRPC, nmCRPC) | Resistance mutation selectivity panel (WT vs. T878A/F876L mutant recombinant proteins) |
| PROTAC / Targeted Degrader | Arvinas (ARV-110), Pfizer, Bristol Myers Squibb | mCRPC (Enzalutamide-resistant) | Ternary complex formation and ubiquitination assays (full-length AR + E3 ligase) |
| N-Terminal Domain (NTD) Inhibitor | ESSA Pharma (EPI-7386), Iterion Therapeutics | mCRPC (AR-V7 positive) | Truncated AR-V7 protein (NTD-only) for binding and functional assays |
| AR-V7 Inhibitor (direct) | ESSA Pharma, Iterion Therapeutics | Enzalutamide-resistant PCa | AR-V7 protein lacking LBD; requires NTD-specific HTS assays |
| Selective Androgen Receptor Modulator (SARM) | Radius Health, GTx | Muscle wasting, Osteoporosis | Tissue selectivity and coactivator recruitment panels |
Key Mutations in AR Drug Resistance
The following clinically relevant AR mutations have been documented (UniProt P10275) and are commonly targeted in drug development:
| Mutation | Clinical Context | dbSNP / VAR ID |
|---|---|---|
| L702H (PAIS) | Partial androgen insensitivity syndrome | rs104894742 / VAR_004679 |
| T878A | Prostate cancer (enzalutamide resistance) | VAR_004680 |
| H875Y | Prostate cancer | rs78686797 / VAR_004681 |
| F876L | Prostate cancer (antagonist-to-agonist conversion) | COSMIC |
| W741L | Prostate cancer (bicalutamide resistance) | COSMIC |