Protein Degraders (PROTACs and Molecular Glues)

As of November 6, 2026, Drugnews tracks 24 clinical-stage protein degraders: 2 approved in the US, 6 in Phase 3, and 15 from Asian companies (12 China, 1 Japan, 1 Taiwan, 1 South Korea).

What these drugs do

A conventional targeted drug blocks a disease protein. A degrader removes it. A PROTAC binds the target with one end and recruits an E3 ligase with the other, so the cell's own disposal system breaks the protein down. A molecular glue is a single small molecule that makes an E3 ligase stick to a protein it would not normally touch.

Removing a protein, rather than blocking it, opens targets that have no druggable pocket and can get around resistance mutations.

2026: degraders reach the market

In May 2026 the US FDA approved Arvinas and Pfizer's VEPPANU (vepdegestrant) for ESR1-mutated, ER+/HER2- advanced breast cancer, the first PROTAC on the market. In August, BMS's ZENBEXUS (iberdomide), combined with daratumumab, received accelerated approval in multiple myeloma as the first CELMoD molecular glue. With both degrader mechanisms approved in the same year, the question has moved from whether degraders can become drugs to who reaches approval first on each target.

Phase 3 activity sits in two areas:

• Blood cancers: BTK degraders from BeOne (tacabrutideg) and Nurix (bexobrutideg), both now in head-to-head Phase 3 trials against pirtobrutinib; and BMS's mezigdomide and golcadomide following iberdomide in myeloma and lymphoma.
• Hormone receptors: ER (vepdegestrant) and AR (BMS-986365 in Phase 3; Novartis's luxdegalutamide in Phase 2).
• KRAS, long considered hard to drug: Astellas's setidegrasib, a KRAS G12D degrader, has started Phase 3 trials in pancreatic and lung cancer.

Asia: China leads on numbers, AR is the most crowded target

China accounts for 12 of the 15 Asian clinical assets. Two Asian assets are in Phase 3: BeOne's tacabrutideg (BTK, three Phase 3 trials under way) and Astellas's setidegrasib (KRAS G12D).

The androgen receptor (AR) is the most crowded target in Asia, split into two different businesses:

• Oral AR degraders for prostate cancer: Hinova's HP518, Qilu's QLH12016 and Hengrui's HRS-5041, up against late-stage assets from BMS and Novartis.
• Topical AR degraders for hair loss and acne: Kintor's GT20029 and Taiwan-based AnHorn Medicines' AH-001, the only two topical AR degraders in the clinic.

The topical approach targets a different problem. Androgenetic alopecia needs long-term treatment, and oral anti-androgens act throughout the body. A topical degrader is designed to remove AR locally in the scalp.

The two companies took different routes. Kintor started in China: it reported a positive Phase 2 in androgenetic alopecia in April 2024, met the primary endpoint of a Phase 2 in acne in August 2025, and has completed a US Phase 1. AnHorn started in the US: AH-001 has completed a US Phase 1 single- and multiple-ascending-dose study, is preparing for Phase 2, and is seeking global licensing and co-development partners.

Taiwan's position

AnHorn's AH-001 is currently Taiwan's only clinical-stage protein degrader, and it is on a US clinical path. AnHorn has also integrated NVIDIA BioNeMo and its in-house AI platform AIMCADD into its drug development process for degrader design.

What to watch

• Phase 3 results for tacabrutideg and bexobrutideg against pirtobrutinib, which will show whether BTK degraders can replace BTK inhibitors.
• The BMS-986365 Phase 3, which will set the position of AR degraders in prostate cancer.
• Topical AR degraders: Kintor's next GT20029 trial and the start of AnHorn's AH-001 Phase 2.