Rong Yun has integrated the whole database, combing the acceptance of domestic 1 new drug applications, the targets involved and the latest research and development progress during the period of 20 16-202 1. And classify them, sort out the history of hot targets, the statistics of target distribution of new drugs in the main treatment fields in recent 6 years, and the latest research and development progress of the five hot targets in the world; Based on the index above IND of innovative drugs in the world and China, the most potential "China New" index was screened out. ...
Finally, the above contents are organized into "China? White paper on the target of the first kind of new drugs.
First, the number of new drugs accepted in China has increased year by year.
During the statistical period of 20 16-202 1, the number of applications for domestic 1 new drugs showed a continuous growth trend, with the compound annual growth rate (CAGR) of applications as high as 40%. Among them, the number of applications accepted increased by 83% in 2020, the largest increase compared with the past, reflecting the great improvement of CDE efficiency and market activity; In 20021year, the number of domestic applications for a class of new drugs continued to increase, and the number of applications increased by 68% compared with 2020, reaching 1379.
"China medical Rong Yun? Me? White paper on new drug targets
2. 202 1 New drugs listed in China achieved excellent results.
In 20021year, China's innovative pharmaceutical industry made great strides, the independent research and development capabilities of local pharmaceutical companies continued to improve, and the number of new drugs listed in China reached a new high, reaching the highest level in the past six years. According to statistics, in 20021year, there were 25 domestic new drugs listed in China, including 8 chemical drugs1year and 7 biological drugs. In the past six years, these two kinds of drugs have been listed in the corresponding categories with the largest number.
In 2002 1 year, there were1new drugs (chemicals) listed in China.
"China medical Rong Yun? Me? White paper on new drug targets
In 2002 1 year, there were1new drugs (biological drugs) listed in China.
"China medical Rong Yun? Me? White paper on new drug targets
From the perspective of chemical medicine, the research and development of pharmaceutical companies is in full bloom, involving a comprehensive range of fields and objects.
From the perspective of biopharmaceuticals, the research and development of pharmaceutical companies shows signs of clustering, focusing on a disease field.
From the enterprise's point of view, there are three kinds of medicines in jiangsu hengrui, namely, Daxi, Proline Gliclazide and Hainazine. Followed by Rongchang creatures, there are two kinds of * *, namely vidicon and tetasip. The rest of the enterprises have one.
Antitumor drugs and immunomodulatory drugs are favored in this field.
China has a huge tumor market. According to yost Sullivan's data, there were 4.4 million new cancer patients in China in 20 19, and it is expected to reach 5 million in 2024. In view of a large number of unmet medical needs in the field of cancer, a large number of pharmaceutical companies will focus on the research and development of cancer drugs. According to statistics, in 20021year, 37.5% of the global drug research and development pipeline was occupied by tumor drugs.
Judging from the ranking of domestic biopharmaceuticals listed in 20021,pharmaceutical companies have invested the most in the field of anti-tumor drugs and immunomodulatory drugs, with 7 layouts, accounting for 39% of all disease fields.
From the chemical diagram of domestic new drugs listed in 20021,pharmaceutical companies are all aiming at the field of anti-tumor and immunomodulatory drugs, and are doing research and development in this field.
It can be seen that the domestic new drugs listed in 20021,whether biological drugs or chemical drugs, pharmaceutical companies prefer the field of anti-tumor and immune function regulation diseases, on the one hand, because there are many unmet clinical needs in this field, which is of great research and development value; On the other hand, there may be herd mentality at work. However, it is not yet possible to generalize whether the trend of following R&D is catching the wind or hitting the gun. The national policy advocates that pharmaceutical companies refuse to blindly follow the trend of new drug research and development, and advocates and encourages patient-oriented differentiated innovation. Pharmaceutical companies may achieve better results by investing in research and development in this regard.
PD-L 1 the goal is a complete victory.
Among the domestic new drug targets listed in 20021,PD- 1\L 1 is the most (biopharmaceuticals), and * * * has four kinds, two of which are sugelizumab and envolizumab, and the Cepali monoclonal antibody and Pai Ampley monoclonal antibody have been approved one after another this year. PD- 1\L 1 target is the most popular target for pharmaceutical companies in recent years, especially PD-L 1. According to statistics, PD-L 1 target has enterprise layout in the fields of monoclonal antibody, double antibody and small molecule drug. During the statistical period, the number of new drug applications increased gradually, and the number of new drug applications for the first time in 202/kloc-0 reached 24. At present, there are 55 drugs targeting PD-L 1 * *, two of which have been listed, and all of them will be listed this year. There are still four models that have applied for listing. ...
PD-L 1 target drug development stage
"China medical Rong Yun? Me? White paper on new drug targets
Iii. 202 1 List of new drugs listed in China.
Chemicals:
0 1 ? Darsili
Drug name: dalsley hydroxyethyl sulfonate tablets
Product name: Airikang
R&D enterprise: jiangsu hengrui Pharmaceutical.
Target: CDK4CDK6
Time to market: 202165438+February.
First indication: metastatic breast cancer
Introduction: Dalcy is the first CDK4/6 inhibitor developed in China. As a new type of highly selective inhibitor, Darceli has made innovations in the molecular structure of drugs. It can reduce the phosphorylation level of retinoblastoma protein downstream of CDK4 and CDK6 signaling pathways, induce G 1 phase arrest, and thus inhibit the proliferation of tumor cells. The marketing of this drug provides a new treatment option for breast cancer patients.
02 ? Proline constant gliclazide
Drug Name: Proline Hahnge Liner Tablets.
Product name: Qin Rui
R&D enterprise: jiangsu hengrui Pharmaceutical.
Target: SGLT2
Time to market: 202165438+February.
The first sign: type 2 diabetes
Brief introduction: Hahnge Liner is the first innovative SGLT2 inhibitor in China, which can reduce blood sugar by inhibiting the reabsorption of glucose by kidney, reducing the reabsorption of filtered glucose by renal tubule and increasing urine glucose excretion. It is approved that Proline Hahnge Liner Tablets are suitable for improving blood sugar control in adult patients with type 2 diabetes.
03 ? Ethylenediamine citrate tetraacetic acid
Drug Name: Edenafil Citrate Tablets
Trade name: Alex
R&D enterprise: Yuekang Pharmaceutical
Target: PDE5
Time to market: 202165438+February.
First indication: erectile dysfunction
Introduction: Alice Edenafil Citrate Tablets is the first original and innovative anti-ED drug 1. 1 in China. The clinical trial was led by Guo Yinglu, an academician of China Academy of Engineering. Alice has a brand-new chemical structure, specially designed for men in China, with the characteristics of good safety, high efficiency, quick response, small dosage and excellent dosage form. And has patents in 22 countries and regions around the world.
04 ? Omacycline
Drug name: omacycline toluene sulfonate for injection; Omacycline mesylate tablets
Product name: cowboy music
R&D Enterprise: Zaiding Medicine (Shanghai)
Target: 30S subunit
Time to market: 202165438+February.
First indication: bacterial skin infection and bacterial pneumonia.
Introduction: Omacycline mesylate is a new type of antibiotic, which aims to overcome tetracycline resistance and has broad-spectrum antibacterial activity, including Gram-positive bacteria, Gram-negative bacteria, atypical pathogens and various drug-resistant strains. The medicine has two dosage forms: oral and intravenous drip, once a day. Approved for the treatment of community-acquired bacterial pneumonia (CABP) and acute bacterial skin and skin structure infection (ABSSSI).
05 ? Orobatinib
Drug Name: Orobatinib Tablets
Product name: Nilik
R&D enterprise: Guangzhou Shunjian Biomedical Technology Co., Ltd.
Target: ABLBCR；; equipment
Time to market: 202 1 1 1 month.
First indication: chronic myeloid leukemia
Oromotinib is the second third generation BCR-ABL tyrosine kinase inhibitor in the world and the first in China. It can be used to treat adult patients who are resistant to any tyrosine kinase inhibitor and diagnosed as chronic or accelerated chronic myeloid leukemia T3 15I mutation by fully verified detection methods.
06 ? Siglezon sodium
Drug name: sitagliptin sodium tablets
Trade name: Shuangluoping /Bilessglu
R&D enterprise: Chengdu Weixin Pharmaceutical Co., Ltd.
Objective: PPARαPPARγPPARδ
Time to market: 202 1 10 month.
The first sign: type 2 diabetes
Brief introduction: Sigliclazide sodium is an innovative drug with independent intellectual property rights independently developed by China. It is a complete agonist of peroxisome proliferator-activated receptor (PPAR), which can simultaneously activate three subtypes (α, γ and δ) of PPAR, induce the expression of downstream target genes related to insulin sensitivity, fatty acid oxidation, energy conversion and lipid transport, and inhibit the phosphorylation of PPARγ receptor related to insulin resistance. Single drug is suitable for diet control and exercise, which provides a new treatment choice for adult patients with type 2 diabetes.
07 ? Azvudine
Drug Name: Afuddin Tablets
Product name: \
R&D enterprise: Henan Ruier Biotechnology Co., Ltd.
Target: HIV-1; RTVIF
Time to market: July 202 1
The first sign: HIV infection
Introduction: Avdine is a new nucleoside reverse transcriptase and helper protein Vif inhibitor. Compared with lamivudine, the drug activity of afudine is good 1000 ~ 2000 times. The drug can be used in combination with nucleoside reverse transcriptase inhibitors and non-nucleoside reverse transcriptase inhibitors to treat adult HIV- 1 infected patients with high viral load.
08 ? Hai Mai Bo bu
Drug name: Haibomai patch
Product name: Seth May
R&D enterprise: Zhejiang Haizheng Pharmaceutical
Target: NPC 1L 1
Time to market: June 202 1
First indication: hypercholesterolemia
Brief introduction: Haibomai patch is the first cholesterol absorption inhibitor with independent intellectual property rights in China, and it is also the only approved 1 innovative drug in cardiovascular field in China in recent years. 2002/kloc-0 was included in the national medical insurance drug list on February 3, 2002, which brought new choices and hopes to the majority of patients with primary hypercholesterolemia in China.
09 ? Ainovelin
Drug name: enoverine tablets
Product name: Ebond
R&D enterprise: Jiangsu Aidi Pharmaceutical
Target: HIV-1rt.
Time to market: June 202 1
The first sign: HIV infection
Introduction: Enoverine is a non-nucleoside reverse transcriptase inhibitor of HIV- 1 and the first anti-HIV oral drug approved for marketing in China. Inhibition of HIV- 1 replication by non-competitive binding with HIV- 1 reverse transcriptase. The drug is used in combination with nucleoside antiretroviral drugs to treat adult patients infected with HIV-/kloc-0. The listing of this variety provides a new treatment option for HIV- 1 infected people.
10 ? Amitinofovir
Drug Name: Amitinofovir Tablets
Product name: Hengmu
R&D enterprise: Jiangsu Haosen Pharmaceutical
Target: RT
Time to market: June 202 1
First indication: hepatitis B virus infection.
Brief introduction: Amitenofovir is an innovative drug independently developed in China, and it is also the second substitute of Norfovir, belonging to nucleoside reverse transcriptase inhibitors. Tenofovir has been verified by a large number of hepatitis B patients around the world. Its advantage is strong drug effect, corresponding to 8 virus orders of magnitude. So far, there is no report of drug resistance, and it has a good effect in preventing liver cancer and is widely used in people. The listing of this variety provides a new treatment option for patients with chronic hepatitis B.
1 1 ? Sevotinib
Drug Name: Sevotinib Tablets
Trade name: Varysa /ORPATHYS
R&D enterprise: Hutchison Whampoa
Target: c-Met\HGFR
Time to market: June 202 1
First indication: metastatic non-small cell lung cancer
Introduction: Sevotinib is a highly selective oral MET inhibitor independently innovated in China, and it is also the first approved MET targeted drug in China. The medicine is used for adult patients with locally advanced or metastatic non-small cell lung cancer, who have advanced diseases after platinum-containing chemotherapy or are intolerant to standard platinum-containing chemotherapy, and have the mutation of exon 14 of interstitial-epithelial transforming factor (MET).
12 ? Hequ wave pa ethanolamine
Drug Name: Haitu Paethanolamine Tablets
Product name: Hengqu
R&D enterprise: jiangsu hengrui Pharmaceutical.
Target: TpoR
Time to market: June 202 1
First indication: thrombocytopenia, aplastic anemia, idiopathic thrombocytopenic purpura.
Introduction: Hatroppa ethanolamine is an innovative drug 1 independently developed by Hengrui Pharmaceutical Co., Ltd., which is a small molecule nonpeptide thrombopoietin receptor (TPOR) agonist absorbed orally. The drug is mainly used to treat chronic primary immune thrombocytopenia (ITP) with poor curative effect of glucocorticoid drugs, immunoglobulin or splenectomy. It was officially included in the medical insurance catalogue in 2002165438+February.
13 ? Donafenib tosylate
Drug Name: Donafenib Toluene Sulfonate Tablets
Product name: Zepsen/Zepsen
R&D Enterprise: Suzhou Zejing Biotechnology
Target: receptor? Protein tyrosine? Kinase; ? Royal Air Force (RAF)
Time to market: June 202 1
First indication: hepatocellular carcinoma
Introduction: Donafenib is an oral multi-target and multi-kinase inhibitor small molecule anti-tumor drug developed by Zejing Pharmaceutical Co., Ltd., which belongs to 1 class, and the company has independent intellectual property rights. For patients with unresectable hepatocellular carcinoma who have not received systematic treatment before.
14 ? Kangtaisongamine
Drug name: Kangdisoniamide tablets
Product name: Youxitai
R&D enterprise: Monk Medicine
Target: 50-something? Ribosome? element
Time to market: June 202 1
First indication: complex skin tissue infection
Introduction: Condizontamide tablets are innovative drugs with independent intellectual property rights independently developed by China. It is a new generation of oxazolidinone original research drug independently developed by Monk Pharmaceutical Co., Ltd. (No.:1) and approved for listing. It is a major breakthrough of domestic innovative drugs in the field of infectious diseases. It can be used to treat complex skin and soft tissue infections caused by Staphylococcus aureus (methicillin-sensitive and drug-resistant strains), Streptococcus pyogenes or Streptococcus agalactiae, which are sensitive to Contizontamide.
15 ? Levo-ornidazole disodium phosphate
Drug name: disodium levoornidazole phosphate for injection
Product name: Xinrui
R&D enterprise: Huachuang synthesis of pharmaceuticals; Yang Zijiang Pharmaceutical; Jiangsu Hengyi Pharmaceutical;
Target: DNA
Time to market: May 202 1
The first sign: bacterial infection
Introduction: Disodium phosphate of L-ornidazole belongs to nitroimidazole antibiotics, is the sodium salt of phosphate derivative of L-ornidazole isomer, and is the prodrug of L-ornidazole in the market at present. This is the company's first innovative drug, which is mainly used to treat a variety of diseases caused by anaerobic bacterial infections such as Streptococcus, Eichhornia actinomycetes, Porphyrin gel cells, Bacteroides fragilis, Clostridium perfringens and Prudential melanin. At the same time, it can also be used to prevent infection before operation and treat anaerobic infection after operation.
16 ? Pambali
Drug Name: Pambali Capsule
Product name: Bai Huize
R&D Enterprise: Baekje Shenzhou
Target: parp-2; PARP 1
Time to market: April 202 1
First indication: fallopian tube cancer, ovarian tumor and peritoneal tumor.
Introduction: Pambali Capsule is a new generation of PARP inhibitor anticancer drug independently developed by Baekje Shenzhou scientists. It can be used to treat patients with recurrent advanced ovarian cancer, tubal cancer or primary peritoneal cancer with embryo BRCA(gBRCA) mutation who have received second-line or above chemotherapy. Pampali capsule is also the second and fourth approved PARP inhibitor targeted therapy for ovarian cancer in China. The first three drugs are Olapali, NiRapali and Fluzopali.
17 ? Youti Delong
Drug Name: Youdelong Injection
Product name: Youtiti
R&D Enterprise: Beijing Huahao Zhongtian Biotechnology
Objective: tubulin
Time to market: March 202 1
First indication: metastatic breast cancer
Introduction: Utterone is the first innovative anti-tumor drug of epothilone in China, which can promote tubulin polymerization, stabilize microtubule structure and induce apoptosis. Ortazone injection combined with capecitabine is used for patients with recurrent or metastatic breast cancer who have received at least one chemotherapy regimen in the past. The marketing of this variety provides a new treatment option for patients with advanced breast cancer.
18 ? Formitinib mesylate
Drug Name: Fumitinib Mesylate Tablets
Trade name: Aisha
R&D enterprise: Shanghai Alice Medical Technology Co., Ltd.
Target: EGFR
Time to market: March 202 1
First indication: metastatic non-small cell lung cancer
Brief introduction: Fumitinib mesylate tablets are the third generation EGFR-TKI independently developed by Alice Medicine, which belongs to small molecule targeted drugs and is the core product of the company at present. It is suitable for the treatment of adult patients with locally advanced or metastatic non-small cell lung cancer (non-small cell lung cancer), who developed diseases before or after treatment with epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (TKI) and were confirmed to have EGFR T790M mutation. The drug is also planned to be included in the breakthrough treatment variety, and the indication is the first-line treatment of non-small cell lung cancer.
Biomedical Science
0 1 ? Shu grimma
Drug Name: Sulglimab Injection
Product name: Zejiemei
R&D enterprise: Jishi Pharmaceutical
Technology: Monoclonal antibody
Target: PD-L 1
Time to market: 202165438+February.
First indication: metastatic non-small cell lung cancer
Introduction: Sugarlizumab injection is a recombinant anti-PD-L 1 fully humanized monoclonal antibody, and it is the second and fourth approved PD-L 1 monoclonal antibody in China. By eliminating the immunosuppressive effect of PD-L 1 on cytotoxic T cells, it plays an anti-tumor role. The drug is suitable for the first-line treatment of metastatic non-squamous non-small cell lung cancer patients with negative epidermal growth factor receptor (EGFR) gene mutation and anaplastic lymphokinase (ALK) combined with pemetrexed and carboplatin, and the first-line treatment of metastatic non-small cell lung cancer patients combined with paclitaxel and carboplatin.
02 ? Envolizumab
Drug name: envolizumab injection
Trade name: Envida
R&D enterprise: Sichuan Lu Si Kangrui Pharmaceutical Co., Ltd.
Technology: Monoclonal antibody
Target: PD-L 1
Time to market: 202 1 1 1 month.
First indication: advanced solid tumor and metastatic colorectal cancer.
Introduction: Envolimab injection is an innovative PD-L 1 antibody drug independently developed by Corning Jerry. It became the first domestic PD-L 1 inhibitor and the first subcutaneous injection of PD-(L) 1 inhibitor in the world. According to public information, envolimab injection belongs to the fusion protein of PD-L 1 single domain antibody Fc. Based on its unique design, it has advantages in safety, convenience and compliance. Patients do not need intravenous drip, and the medical expenses are low.
03 ? Reggie Olense
Name of drug: Regasai injection
Product name: Benoda
R&D enterprise: Yao Ming Junuo
Technology: CAR-T cell therapy?
Target: CD 19
Time to market: September 202 1
First indication: diffuse large B-cell lymphoma
Introduction: Reggiorensai is the first commercial product of Yao Ming Junuo and the second CAR-T product approved in China after Akirensai. As a CAR-T cell therapy targeting CD 19, reggacoside obtained the first indication for third-line treatment of diffuse large B-cell lymphoma (DLBCL) in China.
04 ? Sepalizumab
Drug Name: Cefalizumab Injection
Product name: Yutu
R&D enterprise: Guangzhou Yuheng Bio.
Technology: Monoclonal antibody
Target: PD- 1
Time to market: August 202 1
First indication: Hodgkin's lymphoma
Introduction: Cepalimab injection was commissioned by Yuheng Bio to be developed by Yao Ming Bio, and it was the first in China to use the international advanced transgenic rat platform (OmniRat? ) Fully humanized anti-PD- 1 monoclonal antibody developed by ourselves. On August 30th, 20021,according to the announcement of National Medical Supplies Administration (NMPA) in official website, the saipalimab injection declared by Guangzhou Yuheng Biotechnology Co., Ltd. was officially approved for marketing, which was used to treat recurrent or refractory classic Hodgkin's lymphoma above the second line.
05 ? Pai Ampley monoclonal antibody
Drug name: Pai Ampley monoclonal antibody injection.
Product name: Anico
R&D enterprise: Zheng Da Tianqing Kangfang (Shanghai)
Technology: Monoclonal antibody
Target: PD- 1
Time to market: August 202 1
First indication: Hodgkin's lymphoma
Introduction: Pai Ampley monoclonal antibody is a recombinant humanized anti-PD- 1 monoclonal antibody independently developed by Kangfang Bio. It is the only novel PD- 1 monoclonal antibody that adopts IgG 1 subtype and is modified by Fc segment. Its antigen binding and dissociation speed is slow, and its crystal structure analysis shows that it has a unique binding epitope, which can block the binding of PD- 1/PD-L 1 for a long time. It can be used to treat adult patients with recurrent or refractory classic Hodgkin's lymphoma (r/r cHL) who have received at least second-line systemic chemotherapy.
06 ? Vidisituzumab
Drug name: Veriximab for injection
Product name: Eddie
R&D enterprise: Rongchang Bio; Yantai Rongchang Pharmaceutical;
Process technology: ADC
Objective: tubulin; ? HER2
Time to market: June 202 1
The first indication: metastatic gastric cancer
Brief introduction: Videcituzumab is an anti-HER2 antibody coupling drug independently developed by Rongchang Bio, and the first ADC independently developed by China Company. It is suitable for the treatment of patients with locally advanced or metastatic gastric cancer (including adenocarcinoma of gastroesophageal junction) who have received at least two kinds of systematic chemotherapy. 202 1 early July, vidiximab was officially released nationwide. According to the data of Rong Yun, before the medical insurance negotiation, the price of this product was 60mg/ piece/box, corresponding to13,500 yuan/box. After entering the medical insurance catalogue, 3800 yuan/box.
07 ? Tetaspu
Drug Name: Tetasip for Injection
Product name: Taiai
R&D Enterprise: Rongchang Biology
Technology: fusion protein; monoclonal antibody
Target: BAFF/BLyS；; April
Time to market: March 202 1
First indication: systemic lupus erythematosus
Brief introduction: Tetasip for injection is the world's first dual-target biological drug independently developed by Rongchang Bio to treat autoimmune diseases such as systemic lupus erythematosus (SLE) and rheumatoid arthritis. This variety is recommended for priority examination and approval. It took 23 days from the marketing application of165438+1October 13 to the priority review, on the grounds that the drug was innovative and had obvious therapeutic advantages.
Four. Prediction of domestic new drug competition pattern in 2022
During 20 16-202 1, with the reform of medical policy, the government encouraged the research and development of innovative drugs, and pharmaceutical companies also entered the innovative drug market in a responsive layout. The number of domestic new drugs in China is on the rise, and major pharmaceutical companies have also achieved good results. The domestic innovative drug market is excellent. It is expected that the domestic innovative drug market will continue to expand in 2022, full of opportunities and challenges.
According to the combined analysis of medical policy and domestic new drug market, it is predicted that the competition pattern of new drugs in 2022 will mainly be in the following aspects:
1, differentiated innovative drugs to avoid serious homogenization competition.
2, according to the policy to protect people's livelihood, improve patients' access to innovative drugs.
3. Innovative drugs that meet unmet clinical needs, such as tumor and neurology, are all unmet clinical needs.
4. Innovative drugs for hot areas and hot targets.
5, the real Mebetter drugs, the real source of innovation or more therapeutic drugs.
6. The goal of "China New" has great research value.