Talk about the current situation of the research and development of hypertension drugs.

China's large population of hypertension patients, currently more than 270 million people, in 2013 by hypertension brought about by the direct economic burden of 210.3 billion yuan, accounting for 6.61 percent of China's total health costs.
has created a huge national health burden.
According to the 2018 Revision of the China Guidelines for the Prevention and Control of Hypertension, the main risk factors for hypertension in the Chinese population include: high sodium, low potassium diet, overweight and obesity, excessive drinking, long-term mental stress and age, family history of hypertension, lack of physical activity, and diabetes, abnormal blood lipids and other causes.
as part of the pharmaceutical industry, today we are simply revisiting the classification and research status of hypertension drugs.
, the number of antihypertensive drugs that have been listed worldwide is large, mainly based on the traditional antihypertensive mechanism.
FDA represents the international standards and levels of new drug development. By combing through the FDA approved antihypertensive drugs over the years, it can be seen that the development of conventional antihypertensive drugs peaked in the 1980s and 1990s, in 20 years a total of 40 antihypertensive drugs were approved, and before the 1980s, because basic medical research on hypertension is still in the accumulation stage, is the accumulation period of antihypertensive drug research and development;
the slowdown in antihypertensive drug research may be mainly related to the slow progress of basic medical research on hypertension, the increased cost of developing new drugs, and the decrease in clinical benefits and market share. table
1 Hypertension drugs after decades of development, antihypertensive drugs from the early diuretics, β-blockers, calcium antagonists and angiotensin conversion enzyme inhibitors (pri class), to angiotensin blockers (saltan class).
sartan drugs have become the most widely used anti-depressants because of the advantages of more thorough anti-depressant effect, fewer side effects, long ller effect and can be used in tannin-type drugs. Table
2 Classification, structure and deficiency of antihypertensive drugs Due to hypertension often combined with other cardiovascular diseases, the condition is very complex, patients need long-term medication, while a variety of antihypertensive drugs taken at the same time, exacerbating the patient's compliance with the drug problem.
based on the current situation and clinical needs of antihypertensive treatment, the current research and development of antihypertensive drugs mainly to new drugs, slow-control release technology, fixed compound preparations in the three directions.
1. Because of the low disclosure of phase I clinical trial information, this section lists only drugs that are in Phase 2,3 clinical trials.
(1) Phase III clinical trial drugs are currently in the study of a smaller number of drugs directly used to lower blood pressure, less drugs in Phase III. clinical trials, of which sparsentan is oral bidirectional ACEI and has a highly selective Eta blocking effect, compared to Ebershatan, the product can significantly reduce protein urine level.
TRC-150094 is a silent information regulator 2 isomotherm 1 (SIRT1) astitid, mainly associated with metabolic diseases, not mainly used for hypertension but may be used in comprehensive treatment of hypertension.
(2) Phase II clinical trial drugs in Phase II clinical studies have a large number of drugs: Firibastat is a (first-in-class) hypertension drug, Mitigating the production of angiosin III. is the first BAPAI candidate drug selected by Quantum Genomics, a precursor drug that delivers EC33 products in the brain, which is a selective and specific peptidease A inhibitor, thus preventing the production of angiosin III. in the brain, by inhibiting Amamineptide to play a central antipressure effect without affecting the activity of the outer angioanthrosin system (RAS).
PL-3994 is a heart sodium anthetistant that works in synergy with ACEI to lower blood pressure. It is expected that the clinical use of Praliciguat (IW-1973) in combination with standard antihypotensive therapies is an oral, soluble bird nucleotide cyclase (sGC) stimulant for the potential treatment of diabetic nephropathy and left-room contractional function of remaining heart failure (HFpEF), which can improve blood vessel and metabolic function, and reduce inflammation and fibrosis associated with these diseases, although it has a blood pressure reduction effect, but is mainly used for the treatment of other cardiovascular diseases.
LHW-090 is a membrane metal endopeptase inhibitor, clinical trials showed significant antihypulation effects, and compared with the placebo group did not have significant adverse reactions.
Rosafuroxin is a sodium potassium ion channel conversion enzyme inhibitor that also affects the Src signaling pathway and protects the heart and kidneys while lowering blood pressure.
Vasomera study code-named PB-1046 has good biological activity, clinical trials only need subsuplisive injection 1 time / week to play a better clinical effect.
2. In order to overcome the shortcomings of the short half-life of some antihypertensive drugs and the need to take them multiple times, many companies have developed antihypertensive drugs for slow-release, such as non-lodipine, which are made into slow-release preparations, and patients take fewer medications per day.
3. Fixed compound preparations Fixed compound preparations have several advantages: several drug synergies can improve the effectiveness of blood pressure reduction, reduce the single dose of each drug, reduce its side effects, or make some side effects offset each other, patients' blood pressure decline is more stable.
at the same time, fixed compound preparations help increase patient compliance compared to multiple single drugs.
the past 15 years, many fixed-dose compound drugs consisting of two or more drugs have been approved for market worldwide.
of all two- or three-drug compound products, ammonia chloride is one of the priority drugs.
However, due to the high safety requirements of cardiovascular drugs, clinical trials require more projects, therefore, the development of new antihypertensive drugs, research and development cycle is relatively long, and high costs, risk benefits than large, want to enter the field of pharmaceutical companies to be very cautious, carefully do a good job in the early stage of research and project work.
Refester. Haitong Securities Research Report Jibel: "Research and Marketing" as a whole, multi-product co-exists, Ping An Securities Pharmaceutical Industry Special Report Consistent Evaluation of the second half of the opening: early birds have insects to eat. Feng Hanlin. Advances in the development of antihypertensive drugs . . . Modern Drug Applications in China, 2020, v.14 (04): 234-238. Ma Qianli. The research and development of antihypertensive drugs shows three major trends. China Medical Journal, 2019-08-05 (004).