New Drugs | Inventory of domestic production status of original research new drugs in the first quarter of 2021, 3 new drugs listed in urgent need of clinical overseas new drugs

►Ramucirumab (Cyramza) is a fully human IgG1 monoclonal antibody targeting VEGFR-2 (vascular endothelial growth factor receptor 2).
It is the world's first and so far only approved for gastric cancer The second-line therapy for gastroesophageal junction cancer is also approved for the treatment of NSCLC, colorectal cancer and hepatocellular carcinoma.
In China, Ramucirumab's listing application was accepted by CDE in January 2021, and its expected indications are: second-line treatment of advanced gastric or gastroesophageal junction adenocarcinoma.

Among the three anti-infective drugs, two are antibiotics and one is an anti-HIV compound preparation.

►Eracycline (eravacycline, Xerava) is a new, fully synthetic, broad-spectrum, fluorinated tetracycline, intravenous antibiotic, which prevents bacterial protein synthesis by binding to 30S ribosomal subunits.
It is used for treatment including First-line empirical single-agent treatment for multi-drug resistant bacteria infections including Gram-negative bacteria and Gram-positive bacteria infections.
In 2020, it has been approved in Singapore, the United States and Europe for the treatment of complicated intra-abdominal infection (cIAI) in adults over 18 years of age.
The drug was developed by Tetraphase Pharmaceuticals.
In February 2018, Genting Xinyao signed an exclusive agreement with Tetraphase Pharmaceuticals for US$43.
5 million to obtain the development and commercialization rights of the drug in China, Taiwan, Hong Kong, Macau, South Korea and Singapore .

►Pivmencillin is a double ester of mecillin.
It is well absorbed after oral administration, and is rapidly hydrolyzed in the body into mecillin with antibacterial effect.
Its antibacterial effect is the same as mecillin.

►Dolutegravir and Rilpivirine Tablets is a new two-in-one HIV compound drug.
It is composed of dolutegravir and rilpivirine in a 50mg/25mg specification.
Among them, dolutegravir (DTG) belongs to Integrase chain transfer inhibitors (INSTIs), which block HIV from inserting viral DNA into host CD4 cells.
Ripavirin (RPV) belongs to non-nucleoside reverse transcriptase inhibitors (NNRTIs) and non-competitively inhibits HIV-1 reverse transcription The enzyme thereby inhibits virus replication.
In 2017, the drug was approved by the FDA for use in a stable antiretroviral regimen that has been received for at least 6 months to achieve virological suppression (HIV-1RNA <50 copies/ml) without a history of virological failure, and for any NNRTI or INSTI Adults infected with HIV-1 without known or suspected drug resistance mutations will have sales of up to 639 million U.
S.
dollars in 2020.

The two immune system disease drugs are Pfizer’s Abxitinib tablets and Amgen’s Approst tablets, and their marketing applications have been included in the priority review process.

►Abrocitinib is an oral small molecule selective Janus kinase (JAK) 1 inhibitor, which is used for the treatment of moderate to severe atopic dermatitis (AD) patients aged ≥12 years.
The market application is in Europe and America Enter the review.
In China, its marketing application (acceptance number JXHS2100020/21/22) was accepted by CDE in 2021, and was subsequently included in the priority review.
The indication is combined or not combined with topical therapy, and the treatment is not well or unsuitable for topical therapy.
These treatments for moderate to severe atopic dermatitis patients aged 12 years and older include relief of itching.

►Apreste is a small molecule inhibitor of phosphodiesterase 4 (PDE4), which promotes the increase of intracellular cyclic adenosine monophosphate (cAMP) content by inhibiting PDE4, thereby increasing anti-inflammatory cytokines and down-regulating inflammation.
The drug was developed by Xinji and was approved in the United States in 2014.
It is currently approved for the treatment of adult active psoriatic arthritis (PsA), moderate to severe plaque psoriasis and combined with Behcet For Behcet-related oral ulcers, Xinji purchased the drug for US$13.
4 billion in 2019.
In China, the application for the original research Apster was accepted by the CDE in February 2021, and was subsequently included in the priority review, with the indication for psoriasis.
However, at present, domestic four-price companies have submitted applications for the listing of Apster's generic drugs.

In addition, the market potential of several other original research drugs in the first quarter of 2021 should not be underestimated.

►Opicapone (Ongentys) is a new generation of peripheral catechol O-methyltransferase (COMT) inhibitor, developed by the Portuguese company Bial-Portela, and has been used as a levodopa/dopa decarboxylase inhibitor Adjuvant therapy to treat patients with Parkinson’s disease that cannot stably control motor symptoms due to end-of-dose phenomenon.

►Luspatercept (Reblozyl) is a world's first red blood cell maturation agent, used to regulate late red blood cell maturation.
The drug was jointly developed by Xinji (later acquired by BMS) and Acceleron, and has been approved for the treatment of adult β-thalassemia patients who require regular red blood cell (RBC) transfusion and myelodysplastic syndrome (MDS) with ring Sideroblasts or myelodysplastic/myeloproliferative tumors with ring sideroblasts and thrombocytosis-related anemia.
In China, the drug's marketing application was accepted by CDE in February 2021, and was subsequently included in the priority review for the indication β-thalassemia.

►Finerenone is a potential "first-in-class" non-steroidal selective mineralocorticoid receptor antagonist (MRA).
Its new drug application for the treatment of chronic kidney disease patients with type 2 diabetes is under review in the United States.
In China, the drug's marketing application was accepted by CDE in February 2021.

►Stuximab is an IL-6 monoclonal antibody used to block the activity of the elevated multifunctional cytokine interleukin-6 (IL-6) detected in patients with Castman’s disease.
It has been approved in many countries and regions for the treatment of HIV-negative and HHV-8-negative idiopathic multicentric Castleman disease (iMCD) patients.
The drug was developed by EUSA Pharma.
In 2021, BeiGene obtained the development and commercialization rights of the drug in Greater China.
In China, the drug's marketing application was accepted by CDE and was subsequently included in priority review.

►Tigolasan is a potassium ion-competitive acid blocker introduced by Shandong Luoxin from CJ HealthCare Corporation in South Korea.
It competes with the potassium ion binding site of H+/K+-ATPase (proton pump) in wall cells.
Inhibit gastric acid secretion, CDE accepts its marketing application in January 2021.

Among the 21 new drugs mentioned above, Sony Deji, Aprost, and Stuximab are included in the "List of New Drugs Urgently Needed in Clinics".
At present, with the reform of my country's drug approval system, the time from application to approval of new drugs in China is getting shorter and shorter.
It is expected that more and more new drugs will be approved and published in China as soon as possible to benefit the majority of patients.