Approved Targeted Oncology Drugs
The current standard of care is anchored by several highly successful biotherapeutics that have validated the commercial and clinical viability of complex biologics.
Blockbuster Antibody-Drug Conjugates (ADCs)
ADCs have firmly established themselves as critical Targeted Oncology Drugs in breast cancer and solid tumors:
- Enhertu (trastuzumab deruxtecan): Developed by AstraZeneca and Daiichi Sankyo, Enhertu revolutionized the treatment of HER2-low and HER2-positive breast cancers, generating over $2.3 billion in global sales in 2023.
- Trodelvy (sacituzumab govitecan): Utilizing a topoisomerase payload directed at TROP2, this Gilead Sciences therapy has achieved significant survival benefits in metastatic triple-negative breast cancer (TNBC).
- Kadcyla, Adcetris, and Mylotarg: These legacy approvals remain cornerstone therapies across HER2-positive breast cancer and various hematologic malignancies.
Commercialized Bispecific Antibodies
Bispecific antibodies, which can simultaneously engage two distinct targets, have secured major regulatory approvals:
- Talvey (talquetamab) & teclistamab: In multiple myeloma, these T-cell engagers have demonstrated remarkable response rates by bridging T-cells to GPRC5D and BCMA.
- Columvi (glofitamab): Provides a critical off-the-shelf, fixed-duration treatment option for diffuse large B-cell lymphoma (DLBCL).
- Rybrevant (amivantamab): Acts as a highly effective dual EGFR and MET inhibitor for NSCLC patients with EGFR exon 20 insertion mutations.
Clinical-Stage Targeted Oncology Drugs
The biopharma pipeline is rapidly expanding beyond monospecific targets. The next wave of Targeted Oncology Drugs focuses on bispecific ADCs and dual-payload architectures designed to overcome resistance and combat tumor heterogeneity.
Next-Generation Bispecific ADCs
Several high-profile programs are actively advancing through clinical evaluation in 2026:
- NEOK001 & NEOK002: Developed by NEOK Bio and ABL Bio, NEOK001 is a first-in-class bispecific ADC targeting B7-H3/ROR1, while NEOK002 targets EGFR/MUC1. Both recently secured FDA IND clearance to initiate Phase 1 trials.
- JSKN027: Alphamab Oncology achieved a major milestone by dosing the first patient in a Phase 1 study for this asset, the world’s first bispecific ADC targeting PD-L1 and VEGFR2.
Advanced Bispecifics and Small Molecules
Beyond ADCs, other Targeted Oncology Drugs are showing profound clinical promise. Pumitamig (BNT327), an Fc-silenced PD-L1/VEGF bispecific co-developed by BioNTech and Bristol Myers Squibb, is acting as a next-generation immuno-oncology backbone in late-stage trials. Meanwhile, ArriVent BioPharma’s firmonertinib, a highly brain-penetrant tyrosine kinase inhibitor (TKI), is advancing through global Phase 3 trials for uncommon EGFR variants.
Pipeline Summary
| Drug Candidate | Modality | Target(s) | Current Status |
|---|---|---|---|
| Enhertu | Monospecific ADC | HER2 | Approved / Marketed |
| JSKN027 | Bispecific ADC | PD-L1 / VEGFR2 | Phase 1 Dosed |
| NEOK001 | Bispecific ADC | B7-H3 / ROR1 | Phase 1 IND Cleared |
| Firmonertinib | Tyrosine Kinase Inhibitor | EGFR (Uncommon) | Phase 3 Ongoing |
References
- AstraZeneca (2024). Enhertu Full Year 2023 Sales Results.
- Korea Biomedical Review. ABL Bio, Neok Bio secure US IND clearance.
- ClinicalTrials.gov. U.S. National Library of Medicine Trial Registry.