Targeted Therapy for Non-Small Cell Lung Cancer in China: Latest Developments and Breakthroughs

Non-small cell lung cancer (NSCLC) is the most prevalent and deadliest malignancy in China. In recent years, with the widespread adoption of driver gene testing and the continuous development of targeted drugs, the treatment landscape for NSCLC has undergone a profound transformation. Across driver gene mutations including EGFR, ALK, ROS1, MET, KRAS, and HER2, China has established a comprehensive targeted therapy system spanning from first-generation to third-generation agents, from imported to domestically developed originals — with China leading the way in certain areas.

China has formed a treatment paradigm of "three generations coexisting, with third-generation agents as the preferred choice." From follower to competitor, and now to leader in select domains — Chinese innovative drug companies are rewriting the treatment map for NSCLC.

II. EGFR Mutations — The Main Battleground of Targeted Therapy in China

EGFR mutations are the most prevalent driver gene mutations in Chinese NSCLC patients, occurring at a rate of 30%–50% in East Asian populations. Consequently, EGFR-targeted therapy has long been a top priority in Chinese lung cancer research.

(A) First-Line Therapy: Third-Generation EGFR-TKIs Now Dominant

China now has multiple third-generation EGFR-TKIs approved for first-line treatment of advanced NSCLC with EGFR-sensitive mutations (19del, L858R), including both imported and domestically developed options. These agents have become the standard of care.

(B) Comprehensive Overview of EGFR-TKIs Available in China

The following is a systematic introduction to EGFR-TKIs currently approved or under regulatory review in China.

1. Osimertinib (Tagrisso®) — The Global Benchmark

Osimertinib is a third-generation EGFR-TKI developed by AstraZeneca. It was the first third-generation EGFR-TKI approved globally and remains the benchmark against which others are measured.

Approved Indications in China:

• First-line treatment for locally advanced or metastatic NSCLC with EGFR-sensitive mutations (19del/L858R), based on the FLAURA study
• Second-line treatment for EGFR T790M mutation-positive NSCLC after progression on prior EGFR-TKI therapy
• Adjuvant therapy after curative resection for Stage IB-IIIA EGFR-mutated NSCLC (ADAURA study)
• In June 2026, a new indication was approved — potentially for neoadjuvant therapy in resectable EGFR-mutated NSCLC
• Combination with savolitinib for EGFR-mutated NSCLC with MET amplification after EGFR-TKI progression

2026 CSCO Guidelines: Class I recommendation for adjuvant therapy after surgery in Stage IB-IIIB (T3N2M0) EGFR-sensitive mutation patients; Class II recommendation for uncommon EGFR mutations (S768I, G719X, L861Q) and PACC mutations.

2. Almonertinib (Ameile®) — China's First Homegrown Third-Generation EGFR-TKI

Developed by Hansoh Pharmaceutical, almonertinib is China's first domestically developed third-generation EGFR-TKI.

Approved Indications (5 total):

• Second-line for EGFR T790M-positive NSCLC — Approved
• First-line for EGFR-sensitive mutation (19del/L858R) — Approved
• Adjuvant therapy after surgery — Approved
• Consolidation therapy after radical chemoradiation for locally advanced unresectable NSCLC — Approved
• First-line combination with chemotherapy (pemetrexed + platinum) — Approved January 2026

Key Clinical Data: The AENEAS2 study, published in The Lancet Oncology, demonstrated that almonertinib combined with platinum-based doublet chemotherapy achieved a median PFS of 28.9 months — approximately 10 months longer than the control group — with a 53% reduction in the risk of disease progression or death (HR 0.47).

3. Furmonertinib — Developed by Allist Pharmaceuticals

Furmonertinib is a third-generation EGFR-TKI developed by Shanghai Allist Pharmaceuticals with high selectivity.

Approved Indications:

• Second-line for EGFR T790M-positive NSCLC
• First-line for EGFR-sensitive mutation (19del/L858R)
• Second-line for EGFR exon 20 insertion mutations — approved February 2026

Breakthrough Therapy Designations: January 2026: First-line treatment for EGFR PACC mutations included in CDE's Breakthrough Therapy list. 2026 CSCO Guidelines: Furmonertinib is the only EGFR-TKI simultaneously recommended for both PACC mutations and exon20ins treatment.

Dosing: 240 mg once daily for EGFR exon20ins and PACC mutation advanced NSCLC.

4. Befotertinib (Cymena®) — Developed by Betta Pharmaceuticals

Approved Indications: May 2023 for second-line T790M-positive; September 2023 for first-line EGFR-sensitive mutation. Both indications are included in the National Reimbursement Drug List (NRDL).

5. Rezivertinib (Ruibida®) — Beta Pharma (Shanghai)

Approval Timeline: May 15, 2024 for second-line T790M-positive; November 5, 2024 for first-line EGFR-sensitive mutation. The REZOR study was published in The Lancet Respiratory Medicine. Included in NRDL (2025). 2025 CSCO Class I recommendation.

6. Rilertinib (Shengruisha®) — Nanjing Sanhome Pharmaceutical

Approved June 17, 2024 for second-line; subsequently first-line. Included in NRDL effective January 2025. 2025 CSCO Class I recommendation.

7. Olafertinib (FHND9041) — Under Regulatory Review

Developed by Jiangsu Chuangte and licensed to Henlius. NDA accepted by CDE in February 2026 for first-line EGFR 19del.

8. Asandeutertinib (TY-9591) — First EGFR-TKI Specifically for Brain Metastases — Under Review

Developed by TYK Medicines, specifically designed for NSCLC patients with brain metastases. Included in priority review (Jan 2026); NDA formally accepted (Feb 2026). Pivotal Phase II ESAONA study presented as LBA at ASCO 2026. Phase I results published in JTO showed good safety and significant efficacy, especially in L858R and brain metastases.

9. Limertinib (ASK120067) — Innovent Biologics

Approved for second-line T790M-positive and subsequently first-line EGFR-sensitive mutation. A Phase III trial vs. gefitinib was conducted across 56 Chinese hospitals.

10. Mefatinib (Mairuidong®) — Specifically for EGFR L858R Mutation

Developed by Hangzhou Zhongmei Huadong Pharmaceutical. Approved October 28, 2025 for first-line treatment of EGFR exon 21 L858R substitution mutation. Phase III trial vs. gefitinib met primary endpoint. 2026 CSCO and IV Primary Lung Cancer Chinese Treatment Guidelines both give Class I recommendation. First prescription in China written May 2026.

11. Lazertinib (Leclaza®) — Imported Third-Generation EGFR-TKI

Developed by Yuhan Corporation (Korea). Approved in China for combination with amivantamab for first-line EGFR 19del/L858R. The MARIPOSA study demonstrated superiority of the combination over single-agent targeted therapy. First prescription in China written October 9, 2025.

12. Zorifertinib (Zeruini® — formerly AZD3759) — First-Generation EGFR-TKI for Brain Metastases

Approved November 20, 2024 for first-line treatment of EGFR-sensitive mutation with CNS metastases. It is the first EGFR-TKI specifically developed and approved for NSCLC patients with brain metastases — a historically difficult-to-treat population.

13. Others Under Development or Recently Approved

• Lietinib (Aoyixin®) — Approved January 2025 for second-line T790M; first-line also approved; both in NRDL.
• Dosafertinib (Kadasha®) — Deuterated osimertinib derivative; approved August 2026 for first-line EGFR-sensitive mutation with CNS metastases.

III. ALK Mutations — Domestic Innovations Continue to Emerge

ALK fusion genes are positive in approximately 3%–7% of NSCLC cases. Although the proportion is relatively low, the patient population is substantial and targeted therapy is highly effective.

• Conteltinib (Shouyaoze®) — Approved June 11, 2026. Developed by Shouyao Holdings, it is the first ALK inhibitor approved in granule formulation for first-line ALK-positive NSCLC. Pivotal Phase III showed significant PFS extension.
• Dirolax (Xuanfeining®) — Approved August 22, 2025. Developed by Xuanzhu Biopharma, for first-line ALK-positive NSCLC.

IV. ROS1 Mutations — Chinese Originals Going Global

• Taletrectinib — Approved in China (Jan 3, 2025) and U.S. FDA (June 11, 2025). A next-generation, CNS-active ROS1 inhibitor with activity against G2032R resistance. Received Breakthrough Therapy designations from both agencies.
• JYP0322 — A next-generation highly selective ROS1 inhibitor developed in China; results published in Cancer Cell (April 2026) showing potent activity against G2032R and brain metastases with precise TRK avoidance.
• Repotrectinib (AokaiLe®) — Approved by NMPA May 2024; included in NRDL January 2025.

V. c‑Met Mutations — Precision Targeting of a "Difficult Target"

• Glumetinib — Approved in China and Japan for METex14 skipping mutation. Preclinical tumor inhibition >87.7%.
• Bozitinib (Vanbiri®) — First MET-TKI approved for MET amplification in China (June 30, 2025). KUNPENG study: ORR 48.8%, median OS nearly 14 months in MET-amplified (GCN≥6) patients.
• Savolitinib (Orpathys®) — Converted from conditional to full approval (April 2026) for METex14. Also approved in combination with osimertinib for EGFR-mutated with MET amplification after progression.
• SHR-1826 (Hengrui) — c-Met targeting ADC, included in CDE Breakthrough Therapy list for c-Met overexpressing non-squamous NSCLC after ≥1 prior line.

VI. KRAS G12C — Breaking the "Undruggable" Barrier

As of February 2026, four KRAS G12C inhibitors have been approved in China:

• Fulzerasib (Dabert®) — Aug 2024 (GenFleet/Innovent) — China's first and world's third; included in NRDL Jan 2026.
• Garsorasib — Nov 2024 (Jacobio/Allist).
• Goraleicib (Airuikai®) — May 2025 (Shanghai Allist) — also in NRDL.
• Sotorasib sulfate (Jilemei®) — Feb 2026 (Zhejiang Hangyu).

A KRAS G12C inhibitor plus SHP2 inhibitor combination has received Breakthrough Therapy designation for first-line treatment in PD-L1 <50% patients.

VII. HER2 Mutations — A New Target, New Hope

Zongertinib (Shenghetu®) — Boehringer Ingelheim. Conditionally approved Aug 29, 2025 for post‑systemic therapy; further approved for first-line May 21, 2026. 2026 CSCO added as Class I for second-line.

VIII. Current Treatment Landscape and Future Prospects

(A) Targeted Therapy Has Entered an Era of "Blossoming Diversity"

China's NSCLC targeted therapy now covers EGFR, ALK, ROS1, MET, KRAS, HER2, BRAF, and other driver genes, forming a complete treatment system from common to rare targets, from first-generation to third/fourth-generation agents, and from later-line to first-line therapy.

(B) NRDL Coverage Dramatically Improves Patient Access

The latest NRDL (effective Jan 1, 2026) includes almonertinib adjuvant therapy, fulzerasib, repotrectinib, and many more. This enables more patients to afford precision therapy and offers international patients a cost-effective option.

(C) Future Directions

• Fourth-Generation EGFR-TKIs: HS-10504, leading the pack among domestic fourth-generation agents, is expected to receive approval soon, filling the gap for C797S resistance.
• Rise of ADCs: SHR-1826 (c-Met ADC) and others are expanding targeted therapy boundaries.
• Combination Strategies: KRAS G12C + SHP2, EGFR-TKI + MET inhibitor, and other combinations are under active investigation.
• From "Having Drugs Available" to "Using Them Well": As more innovative drugs enter practice and NRDL, patient survival and quality of life will continue to improve.

Conclusion

China's NSCLC targeted therapy is undergoing a historic transformation from "follower" to "leader." In the EGFR space — the core battleground — China has established a comprehensive treatment system spanning first-generation to fourth-generation agents, from sensitive mutations to rare mutations, and from initial treatment to resistance. In ALK, ROS1, MET, KRAS, and other targets, domestic innovative drugs continue to emerge, with some achieving dual approval in both China and the U.S. and going global.

For international patients, China offers not only world-class targeted therapy but also more competitive pricing and shorter waiting times, making it an increasingly important destination for medical tourism. As one industry observer noted — China has made remarkable progress in EGFR-mutant lung cancer treatment, particularly in solutions for resistance after targeted therapy, where Chinese researchers and companies are leading global research directions.