Targeted drug inventory of thirteen lung cancers already on the market

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  • Time of issue:2018-03-28
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(Summary description)

Targeted drug inventory of thirteen lung cancers already on the market

(Summary description)

  • Categories:Industry news
  • Author:
  • Origin:
  • Time of issue:2018-03-28
  • Views:6

Lung cancer has targeted drug inventory

1. Iressa (Gefitinib)

Iressa is the first generation of EGFR-TKI. China's approved indication is to treat locally advanced or metastatic non-small cell lung cancer (NSCLC) with previous chemotherapy. Clinical use of non-small cell lung cancer with EGFR 19 and 21 mutations is good, and 19 mutations are more sensitive.and 19 mutations are more sensitive.and 19 mutations are more sensitive.and 19 mutations are more sensitive.

2. Tarceva (erlotinib)

Tarceva, and Iressa's first-generation EGFR-TKI, China approved indications for locally advanced or metastatic non-small cell lung cancer (NSCLC) after failing at least one chemotherapy regimen. Clinical use for non-small cell lung cancer with EGFR19, 21 mutations is good, 21 mutations are more sensitive.

3. Afatinib (BIBW2992)

Afatinib, an EGFR-targeting inhibitor, is known as the second-generation EGFR-TKI, and is recommended in the NCCN guidelines with the first-generation (Erissa, Tarceva) TKIs as a clinical trial for patients with advanced NSCLC with EGFR mutations First-line medication. But very different from the first generation of medicine.

(1) The target of afatinib not only targets EGFR, but also inhibits the HER2 gene mutation and ErbB4 signaling pathway. Therefore, for patients with HER2 mutation detected in lung cancer, afatinib can be considered. Targeted medication.

(2) The binding of afatinib to the EGFR tyrosine kinase region is irreversible. Therefore, the effect of afatinib is greater.

(3) In a comprehensive study of LUX2 \ 3 \ 6, it was found that afatinib has significant inhibitory activity on rare EGFR mutations (such as Gly719Xaa, Leu861Gln, and Ser768Ile). This means that patients with this type of mutation have better first-line choice of afatinib.

(4) The current clinical trial of LUX-Lung8 shows that afatinib has clinical advantages for patients with lung squamous cell carcinoma that failed previous treatment, so afatinib has also increased lung squamous cell carcinoma (regardless of EGFR gene mutation or not) than the first generation of TKI Indications for backline treatment.

4. Osimertinib (AZD9291)

Oxitinib, a third-generation EGFR-TKI, has been approved for second-line treatment of patients with advanced non-small cell lung cancer (NSCLC) carrying the EGFR T790M mutation. The EGFR T790M mutation is a common cause of resistance to Iressa and Tarceva. The resistance caused by this is good with 9291.

5. Crizotinib

Crizotinib is an anaplastic lymphoma kinase (ALK) and ROS1 inhibitor. In 2011, the FDA approved crizotinib for ALK-positive locally advanced or metastatic non-small cell lung cancer. In 2016, the FDA approved crizotinib for the treatment of patients with advanced ROS1-positive non-small cell lung cancer. In addition, for patients with C-MET amplification, crizotinib may also benefit. Crizotinib is approved primarily based on clinical trials that achieve an objective response rate of 50% to 61% in patients with advanced ALK-positive non-small cell lung cancer.

The latest FDA approval decision in 2016 is based on the results of a study of 50 patients with ROS1-positive non-small cell lung cancer, whose tumors have extensively metastasized from their primary location. The results showed that tumors shrank or disappeared in 2/3 of the participants. This improvement lasted an average of 18.3 months. During this approval process, crizotinib was awarded breakthrough treatment, priority review status, and orphan drug designation.

6. Alecensa

Alecensa, commonly known as Alectinib (Aretinib), is an oral ALK inhibitor, jointly developed by Sinopharm and Roche, and was first approved in Japan in July 2014 to treat ALK-positive advanced or relapsed non-small cell lung cancer; In December 2015, the FDA approved second-line treatment for ALK-positive non-small cell lung cancer. Aretinib is the choice for ALK-positive patients after taking crizotinib resistance.

Alecensa was approved based on two single-arm clinical trials in patients with metastatic ALK-positive NSCLC who were no longer sensitive to crizotinib treatment, and they received oral Alecensa twice a day . In the first clinical trial, 38% of patients achieved partial tumor reduction in NSCLC, and the effect lasted an average of 7.5 months. In the second clinical trial, 44% of patients achieved partial reduction in NSCLC tumors, and the effect lasted an average of 11.2 months.

7. Opdivo (O medicine)

Opdivo, common name nivolumab (navumab) is a new type of PD-1 inhibitor targeted anti-tumor drug launched by BMS. It is a blockbuster drug that is popular among people from all walks of life. It has been approved for patients with advanced metastatic squamous non-small cell lung cancer since 2014. It is suitable for patients who have platinum-based chemotherapy or whose disease has worsened after chemotherapy.

At the same time, Opdivo can also be used for liver cancer, melanoma, kidney cancer, gastric cancer, esophageal cancer, colorectal cancer, Hodgkin lymphoma, squamous cell carcinoma of the head and neck, bladder cancer (urothelial carcinoma), ovarian cancer, Pancreatic cancer.

8. Keytruda (K drug)

Keytruda, common name Pembrolizumab is a monoclonal antibody against PD1 introduced by Merck, and it is a strong competitor of BMS's Opdivo.

Keytruda was approved for second-line treatment of lung cancer after traditional chemotherapy in October 2015: In October 2016, the FDA approved Keytruda for first-line treatment of non-small cell lung cancer with high expression of PDL1 and no EGFR and ALK mutations. The batch is mainly based on data from a randomized, open, phase III clinical trial called keynote-024.

The keynote-024 study compared the efficacy of Keytruda monotherapy with standard platinum chemotherapy for metastatic squamous (18%) or non-squamous (82%) nsclc. The results showed that patients using Kkeytruda had significantly improved progression-free survival and overall survival compared to standard platinum-based chemotherapy.

At the same time, Keytruda can also be used in small cell lung cancer, melanoma, colorectal cancer, head and neck squamous cell carcinoma, bladder cancer (urothelial carcinoma), triple negative breast cancer, esophageal cancer, pancreatic cancer, cervical cancer, uterus Endometrial cancer.

9. Tecentriq (T drug)

Tecentriq, commonly known as Atezolizumab, is a monoclonal antibody developed against PD-L1 developed by Roche-owned gene Tektronix. PD-L1 is a PD-1 ligand, and therefore it is compatible with PD-1 monoclonal antibody Opdivo Similar to Keytruda, Tecentriq's mechanism is also to block PD-L1 / PD-1 interaction.

In October 2016, Atezolizumab was approved by the FDA for second-line treatment of patients with metastatic non-small cell lung cancer, including patients who have deteriorated and progressed during or after platinum chemotherapy, have EGFR or ALK gene abnormalities, and are ineffective after other targeted treatments. patient.

FDA approval is based on the positive results of two clinical trial studies called POPLAR and OAK: POPLAR is a global, multicenter, open-label, randomized phase 2 clinical trial that evaluates Tecentriq compared to docetaxel Efficacy and safety in treating patients with relapsing locally advanced or metastatic NSCLC. Studies have shown that Tecentriq can significantly improve the median survival of the overall study population compared with docetaxel treatment.

At the same time, Tecentriq can also be used for urothelial cancer, colorectal cancer, triple negative breast cancer, etc.

10. Imfinzi

Imfinzi (durvalumab) has a similar mechanism to T drug. It is a PD-L1 inhibitor introduced by AstraZeneca. On February 16, it was approved by the FDA for the treatment of unresectable tumors and non-progressive stage III non-small cell lung cancer (NSCLC) )patient. This immunotherapy has become the preferred option for reducing cancer progression. This is also the first FDA-approved therapy for this particular NSCLC population to reduce the risk of cancer progression. All patients had no cancer progression after chemoradiation. Durvalumab significantly improved progression-free survival (PFS) compared to placebo, with an average PFS of 16.8 months, compared with 5.6 months for placebo (that is, The risk is 0.52). On May 1, 2017, the FDA approved Durvalumab for the treatment of some patients with locally advanced or metastatic bladder cancer.

11. Cyramza

Cyramza, commonly known as Ramucirumab, is a fully human monoclonal antibody targeting vascular endothelial growth factor receptor 2 (VEGFR2). Its anticancer mechanism is similar to that of Avastin. Inhibits angiogenesis to prevent the proliferation and spread of cancer cells.

12In December 2014, the FDA approved Ramucirumab in combination with paclitaxel for the treatment of diffuse non-small cell lung cancer and NSCLC treated with other targeted drugs for EGFR or ALK mutations.

Approval is based on an international study of 1,253 patients with non-squamous cell and squamous cell non-small cell lung cancer from 26 countries on six continents, and found that Ramucirumab prolonged the overall survival of the placebo group by 1.4 months, except In addition, the median overall survival, average progression-free survival, and overall response rate were significantly improved.

12. Yervoy

Yervoy, commonly known as Ipilimumab (Ipilimumab), is an immunomodulator, also known as an immune node inhibitor. This type of drug activates the immune system by suppressing immune nodes, enabling the immune system to recognize and kill tumor cells .

Yervoy's target is cytotoxic T lymphocyte-associated antigen 4 (CTLA-4). CTLA-4 is an important immune node protein that can down-regulate the immune system (reducing the activity of cytotoxic T lymphocytes), thereby making tumors Cells are prevented from being cleared by the immune system. Ipilimumab turns off this inhibition mechanism so that cytotoxic T lymphocytes can re-identify and kill tumor cells.

Currently, Ipilimumab has multiple clinical studies on lung cancer, including combined nivolumab and traditional chemotherapy drugs for the treatment of small cell lung cancer and non-small cell lung cancer. This drug has a good prospect for treating lung cancer.

13. Avastin

Avastin, commonly known as Bevacizumab (bevacizumab), is an anti-vascular epidermal growth factor A (VEGF-A) monoclonal antibody that inhibits blood vessel growth in tumor tissues and enhances the efficacy of chemotherapy.

In 2006, the FDA approved Bevacizumab for the first-line treatment of advanced non-small cell lung cancer in combination with traditional chemotherapy drugs. This approval is based on a phase III clinical study called E4599. This study shows that after Avastin treatment, the overall survival of patients Improved by 2 months.

The launch of targeted drugs brings the gospel to lung cancer patients, greatly improving the survival and quality of life of patients. However, the application of targeted medicines must be reasonable, well-founded and cannot be used blindly.

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