A complete review of the nine major drug targets for non-small cell lung cancer

As we all know, lung cancer is the "killer" with the highest morbidity and mortality in the world

1.

At present, EGFR-TKI has developed into the fourth generation, and a total of 8 drugs have been launched

The four EGFR inhibitors currently in Phase III clinical trials include two third-generation EGFR inhibitors, FHND9041 from Chia Tai Fenghai and RX518 (olafertinib) from Runxin Bio

2.

About 5.

At present, there are 4 domestic new drugs in clinical phase III for ALK targets, namely CT-707 (Conteltinib, SY-707) from Shouyao Holding, TQ-B3139 from Chia Tai Tianqing, XZP-3621 from Sihuan Medicine and Fuxing.

3.

About 1.

The domestic innovative drug tabratinib has been included in the list of breakthrough therapy drugs by the Center for Drug Evaluation (CDE) of the China National Medical Products Administration (NMPA), as well as cabozantinib, ensatinib, and rebotinib.

4.

About 5.

A number of clinical studies on Gumetinib, Britinib, Cabozantinib, etc.

5.

Current regimens for BRAF V600E include vemurafenib, dabrafenib, and dabrafenib + trametinib

6.

RET fusions occur in approximately 1.
4% of NSCLC patients
.
The NCCN guidelines recommend that the first-line first-line regimen is pilatenib or Selpercatinib; other regimens are vandetanib or cabozantinib
.
Among them, pratinib is the first and only marketed RET inhibitor in China
.

7.
KRAS mutation

At present, there are no approved targeted drugs for KRAS in China
.
The NCCN 2022 V2 guideline recommends AMG510, but because domestic patients are not available, the CSCO guideline recommends referring to the treatment of driver gene-negative NSCLC
.

Fortunately, with the continuous efforts of medical researchers, KRAS, the most difficult target, has finally broken defense.
In addition to AMG510, there are many drugs under development that have achieved early success in the clinical research stage: including: Adagrasib (MRTX849 ), JNJ-74699157 (ARS-3248), JAB-3312, LY3499446 and pan-KRAS inhibitor BI 1701963,
etc.
What's more worth mentioning is that the domestic innovative drug D-1553 has also been officially recruited for various solid tumor patients with KRAS g12c mutation
.

8.
ERBB2/HER2 mutation

About 5.
4% of NSCLC patients have ERBB2/HER2 mutations
.

In addition, afatinib, bocitinib, and TAK-788 are in early clinical studies
.

9.
PIK3CA mutation

At present, there are no approved targeted drugs for PIK3CA in China
.

The most advanced, Alpelisib (BYL719), is a potent and selective PI3Kα inhibitor currently in Phase II clinical studies for the treatment of non-small cell lung cancer
.