Inventory: 25 drugs listed in the antidepressant field from 1980 to 2020

Depression is a common disease that affects more than 264 million people worldwide and the prevalence rate is increasing year by year; Nearly 800,000 people die each year from suicide, which has become the second-largest cause of death among the 15-29 age group.
drug intervention is one of the most important treatments for depression, and dozens of drugs have been approved for sale over the past 60 years, but even so, the current clinical needs have not been met! 1. Antidepressants and FDA-approved phase features In 1959, the FDA approved the first antidepressant drug - propylene, which has been developed in this field for more than 60 years.
Usually, this is considered a cyclical process for redeteing the "new drug-new theory" and can be roughly divided into three stages, i.e. "slow start/side effects are large" - "slow start/side effects are small" - "fast start-up/side effects are small".
Based on the classic "monoamine hypothesis", the first wave of antidepressant development occurred after 1980, especially from the listing of fluoxetine in 1986 to the listing of dolositin in 2004, during which time classic drugs that are still used on the front line have emerged; Since 2016, at least six new drugs have been classified by the FDA as breakthrough therapies or fast-track approvals, with S-ketamine (new dosage form) and brexanolone (postpartum depression) approved by the FDA in 2019.
Figure 1.1 FDA-approved antidepressants - Important time nodes (Photo:) 2, 1980-2020 Nearly 25 antidepressants approved for the global market through statistics, the world has been approved for the market antidepressant varieties More than 60, many of which are no longer mainstream or even withdrawn from the market, are summarized as 25 varieties that have been active in the market for nearly 40 years since 1980, and there are still heavy bomb-grade drugs that sell more than $1 billion a year.
A brief description of the 25 antidepressant varieties can be found in the table below: Table 2.1 has been listed related to antidepressants 3, 25 antidepressants listed varieties of the 25 depressive areas listed from 1980 to 2020, the adaptation aspect is often not limited to depression, its mental areas related anxiety, mania, schizophrenia, etc. are often related accordingly; Many varieties, even though they have been on the market for decades, are still clinically commonly used first-line drugs; in terms of global sales, some are super-heavy bombshell drugs that have created billions of dollars; and statistics on these varieties make it even less difficult to see that pharmaceutical companies that invest in drug development in the field of depression are often large multinational pharmaceutical companies that are still digging deep into new drug discoveries in the field after decades of experience in depression drug development.
Brexanolone (2019) development company for Ligand, later authorized SAGE Therapeutics, approved by the FDA in 2019 for clinical treatment of postpartum depression, is a γ-amino butyric acid A-subject regulator; Epilepsy continues to be in Phase III, primary tremor is in Clinical Phase II, and the drug was approved as an orphan drug and fast-track drug in the United States in 2014 due to primary tremor, and was awarded a breakthrough treatment for postpartum depression by the FDA in 2016.
the dosage form, the variety is intravenous, with a content of 100 mg/20mL per bottle;
Brexpiprazole (2015) development company for Otsuka Pharmaceuticals and Lingbei Pharmaceuticals, approved by the FDA in 2015 for listing; A-and-dethyrene α seedents, with 5-HT1A and D2-subjected partial astitids, are clinically used to treat adult patients with schizophrenia, and are combined with antidepressants to assist in the treatment of adult patients with severe depression.
For patients with severe depression, the recommended starting dose is 0.5 mg or 1 mg once a day, the maintenance dose is 2 mg once a day, and the maximum dose is 3 mg once a day.
PS: Originally brexpiprazole, despite its short time-to-market, has grown to a heavyweight-grade drug in the global market, with global sales of $1.1 billion in 2019>
(2013) development company for Forest, which was approved by the FDA in 2013, is widely regarded as a powerful selective 5-serotonin and demethyl kidney Adenin reuptake inhibitors, which are used to treat severe depression, and three clinical trials have shown that L-Minaplund hydrochloric acid performed better than placebos in improving depressive symptoms and did not show any difference in response to treatment results with age, sex, and race.
2013 development company for Takeda Pharmaceuticals and Lingbei Pharmaceuticals, approved by the FDA in 2013 for listing; Body astrists, 5-HT1B-subjected partial astrists, and 5-HT3, 5-HT1D, 5-HT7-subject antagonists are considered to be the first and only compounds combined with pharmacoetic activity and clinically suitable for severe depression. More than
clinical trials have shown that the overall clinical efficacy scale of voxixitin is significantly better than that of the placebo group, but the complete antidepressant effects of the variety are usually detected at or after week 4, and the time for depression recurrence increases significantly.
PS: the original research products in the Chinese market bid price of about 500-580 yuan / box.
Virazone hydrochloride (2011) development company for forest laboratories, approved by the FDA in 2011, is a 5-serotonin reuptake inhibitor and 5-serotonin (5-HT1A) subject part agonist, used to treat severe depression.
clinically based on four multi-center, randomized, double-blind, placebo-controlled trials, montgomery depression evaluation scale scores were better than those in the placebo group.
Agomelatin (2009) development company for Schweija, approved by the EMA in 2009, approved by the NMPA in 2011, is a 5-HT2C regulator antagonist, but also melatonin ligand 1A and 1B (MT1 and MT2) agitants for the treatment of severe depression.
clinical studies showed that 54.3 percent of patients in the dosage group were respondents, compared with 35.3 percent in the placebo group, while in another study CL3-043, the total HAM-D score was significantly lower than in the placebo group, with 49.1 percent in the Agomelatine group and 34.3 percent in the placebo group.
PS: The winning bid price of the original research product in the Chinese market is about 238 yuan/box.
Devin Lafayette (2008) development company for India Alembic, as early as 2008 approved by the FDA listed, is a 5-serotonin and dethyroid epinephrine reuptake inhibitor, is the main active metabolites of verafasin, mainly used to treat severe depression in adults.
dosage form is an oral slow-release tablet containing 50 mg or 100 mg of Dirafacin per tablet;
Serum acid dextaxin (2008) development company for Pfizer, in 2008 approved by the FDA listed, is 5-serotonin and dethylaphetamine reuptake inhibitor, the drug is suitable for the treatment of severe depression, its dosage form is oral slow release tablets, each tablet contains 50 mg or 100 mg of dexylafacin;
PS: Global sales of the original research firm's amber acid-drenched Rafasin have fallen sharply in recent years, from $700 million in 2015 to nearly $200 million in 2018.
Lothitin (2004) development company for Lilly, was approved by the FDA in 2004 and then approved by the EMA the same year for the treatment of severe depression, widespread anxiety disorder, peripheral nerve pain, fibromyalgia and chronic muscle and bone pain.
treatment for depression, the recommended dose is 20 mg per day, 2 times a day, maintenance treatment, 60 mg per day, 1 time a day.
, this drug is not only used to treat depression, but also to treat stress urinary incontinence, etc.
PS: Global sales of the original variety have declined overall over the past five years, from $1,143 million in 2015 to $725 million in 2019.
Synthon (2003) development company for Synthon, approved by the FDA in 2003, pharmacological effects similar to fluoxetine, is a selective 5-serotonin reuptake inhibitor;
oxalic acid right-hand serotonin (2002) development company for Lingbei Pharmaceuticals, in 2002 approved by the FDA listed, is a selective 5-serotonin reuptake inhibitor, clinically used in adult and 12-17 years of age patients with acute and maintenance treatment of severe depression, and adult patients with extensive anxiety acute treatment.
The developing dosage form of this variety is oral tablets, each tablet containing 5 mg, 10 mg or 20 mg of right-hand cysepopram;
PS: The global sales of the original research varieties in the past 5 years have been relatively stable, both in the range of 400-500 million U.S. dollars;
Aleptide (2002) Development Company for Otsuka Pharmaceuticals, approved by the FDA in 2002 for the dopamine receptor D2, dopamine receptor D3, 5-HT1A receptor part of the agonist, and 5-H T2A subject antagonists; clinically suitable for the treatment of schizophrenia, bipolar disorder, severe depression, dysphoresis, and manic autism; developed dosage forms of 2 mg, 5 mg, 10 mg, 15 mg, 20 mg or 30 mg.
PS: The decline in global sales of original varieties over the past five years has been severe, from $4,074 million in 2015 to $1,228 million in 2019, but it is still a big bomb-grade variety;
astrain (1997) development company for AstraZeneca, approved by the FDA in 1997, approved by the NMPA in 2000 listed, the commodity named Srecon ®; In addition to astraZeneca's agreement to grant Greenlee Pharmaceuticals exclusive, permanent, free, sublicensable trademark licensing rights and other appropriate licenses, as well as the acquisition of the breed's rights in china and other countries and regions, including drug registration certificates, patents, production technologies and commercial materials, and sales networks.
the variety is a double antagonist of type 2 dopamine and 2A serotonin, clinically used to treat schizophrenia, bipolar type I mania, bipolar disorder, depression.
PS: Global sales of the original research varieties have declined significantly in the past five years, from US$1,367 million in 2015 to US$191 million in 2019;
Pfizer (1997/2019) development company was originally Pfizer, first listed in Germany in 1997, is a non-selective N-methyl-D-tiandongine inhibitor (NMDAR) antagonist; 9 Developed by Johnson and Johnson to treat depression, it was approved by the FDA in March 2019 and has been recognized by the FDA for two breakthrough therapies, including the treatment of drug-resistant depression (November 2013) and severe depression at risk of suicide (August 2016).
Redpositin (1997) development company for Pharmacia, first listed in the UNITED Kingdom in 1997, is a selective and powerful dethylamin reuptake inhibitor, while the reuptake of 5-serotonin also has a weak inhibitory effect, with a very low anticholinel activity, After taking the drug will not affect other subjects in the brain, will not play a sedative effect, will not affect the cognitive function of patients, etc. ;
, which is not recommended for older patients, also needs to be phased out to reduce the risk of withdrawal symptoms.
The
hydrochloric acid Minaplun (1996) development company, Pierre Fabre, was first listed in France in 1996 and in China in 2010 as a selective 5-serotonin and epinephrine reuptake inhibitor;
(1993) was approved by the FDA in 1993 for the development of Effexor ® for the treatment of depression.
For patients with moderate depression, a dose of up to 225 mg per day is usually effective, but for patients with severe depression, the dose may need to be increased to 375 mg per day, taken 3 times a day, or 1 dose of slow release preparation per day.
, Verafasin not only has antidepressant effects, but also anti-anxiety effects.
PS: the original research products in the domestic winning bid price of about 100-150 yuan / box (different specifications).
Pfizer," a 1992 development company, was approved by the FDA for sale in 1992 under the name Zloft®; Sherwood is a niamine derivative, an SSRI whose pharmacological effects and uses are similar to those of fluoroxitin; In the treatment of depression, the regular initial dose of Shequlin is 50 mg per day, if necessary, increase the dose of the drug, each increase at least 1 week interval, the increase is 50 mg, the largest amount is 200 mg per day;
PS: the original research varieties in the last 5 years of global sales overall relatively stable, at about 300 million U.S. dollars;