20 13 1 FDA * * approval 1 1 new chemical drugs, including four new molecular solid drugs. In February, new chemical drugs 10 were approved, including 2 molecular entity drugs; In March, new chemical drugs 1 1 were approved, including 4 molecular entity drugs; Eight new chemical drugs were approved in April, and no new molecular entity drugs were found. In May, 8 new chemical drugs were approved, including 4 new molecular solid drugs; Three new chemical drugs were approved in June, and no new molecular entity drugs were found.
There are two types of therapeutic potential, P and S, which are independent of each other, that is, all categories can only contain one letter. Class P: Priority evaluation, treatment breakthrough. Refers to 1) can effectively treat or diagnose a certain disease, and any listed product can give appropriate treatment and diagnosis to the disease; Or 2) improving the treatment of a certain disease more effectively and safely than the products on the market; 3) Compared with the drugs already on the market, it has moderate objective advantages. For example: ① it obviously brings great convenience to patients (such as reducing the number of times of administration), ② it eliminates interference, necessary dangers and side effects, ③ it is effective for diseases of specific groups (such as the elderly, children, or those who are intolerant of the drugs used). Class s: regular review. The therapeutic effect is similar to that of the products already on the market. 20 13 years 1 0-June, the FDA approved 5 1 new drugs, including 37 S-class drugs (routine review), 5 P-class drugs (priority review), orphan drugs1drug, and 9 drugs with unclear therapeutic potential.
20 13, 1-June, the FDA of the United States approved 14 kinds of new molecular substance drugs, including 4 kinds of drugs for treating type II diabetes, 4 kinds of drugs for treating cancer, 2 kinds of contrast agents, drugs for treating multiple sclerosis 1, drugs for treating chronic obstructive pulmonary disease 1, and treatment.
Drugs for treating type I and type II diabetes
1.INVOKANA -SGLT-2 inhibitor
2065438+On March 29th, 2003, US FDA approved the drug invoka na(canaglifozin) developed by Johnson & Johnson Company. Invokana is a selective sodium glucose co-transporter 2 (SGLT-2) inhibitor. SGLT-2 can inhibit the reabsorption of glucose in the kidney, promote the excretion of urine glucose, shift the balance to the direction of energy consumption, and thus reduce blood sugar in the body. There is no risk of weight gain and hypoglycemia, and it is a new drug for treating diabetes. According to its structure, SGLT2 is mainly divided into O- aryl inhibitors, C- aryl inhibitors, S- glycoside inhibitors and N- glycoside inhibitors. At present, O- aryl inhibitors and C- aryl inhibitors are more studied, while the other two types are less studied. Invokana belongs to C- aryl inhibitors.
The clinical research results of INVOKA NA Ⅱ Ⅱ show that the experimental group is better than the control group in reducing the level of A 1C (a commonly used index to measure blood sugar level), and has achieved statistically significant results. The results of phase III clinical trials show that Invokana can effectively improve the blood sugar level of patients and lose weight. The incidence of urinary tract infection in Invokana patients increased, especially the incidence of vaginal candidiasis infection in female patients with type 2 diabetes mellitus increased.
2. Nesina (Agelii) -DDP-4 inhibitor.
201365438+1On October 25th, the US FDA approved Nesina (Agelii Ting), Oseni (Agelii Ting and Pioglitazone Composite Tablets) and Kazano (Agelii Ting and Metformin Composite Tablets) from Takeda Pharmaceutical Company for the treatment of type 2 diabetes. Nesina is a selective dipeptidyl peptidase -IV inhibitor, which is used to improve the blood sugar level of adults with type II diabetes. Dipeptidyl peptidase -IV is a new target for the treatment of type II diabetes, and it is one of the key enzymes that mainly promote the degradation and inactivation of glucagon-like peptide-1 in vivo. Nesina is the fourth dipeptidyl peptidase -IV inhibitor approved by FDA.
Nesina is a unilateral preparation of agliptin, which was first approved by the Japanese Ministry of Health, Labor and Welfare in April 20 10, and was listed in Japan in June 20 10. Takeda Company has twice submitted to FDA for approval, but both of them were rejected because it may lead to organ diseases such as heart disease. The approval of Nesina will make up for the impact on the company caused by the expiration of another diabetes drug Actos patent to some extent. The FDA requires five post-marketing studies on the treatment of nesina: a cardiovascular outcome trial; Strengthen the pharmacovigilance program to monitor liver abnormalities, severe pancreatitis and severe allergies; According to the Pediatric Research Equity Act, three pediatric studies were conducted, including a dose exploration study and two safety and efficacy studies (one was treated with Nesina only, and the other was treated with Nesina and metformin).
Second, tumor drugs
1. multiple myeloma drug-pomace (polidocamine)
20 13 On February 8th, the FDA of the United States approved Pomalyst, a multiple myeloma drug developed by Searle Gene Company, to treat patients with multiple myeloma who still have disease progression after receiving at least two treatments (including lenalidomide and bortezomib), and who have no response to the treatment and have disease progression within 60 days after the last treatment. Pomalyst, a derivative of thalidomide, is the third kind of immunomodulatory drug approved after lenalidomide and thalidomide. Pomalyst is the most effective of the three drugs, with a dose of 4mg per day 1 time, compared with 25mg for nadamide and 800mg for Thalidomide. Phase III study of Pomalyst showed that Pomalyst combined with low-dose dexamethasone can significantly prolong the survival time of patients with refractory multiple myeloma, including patients receiving high-intensity pretreatment, and this combination therapy has the same benefits for patients with lenalidomide and bortezomib resistance. Pomalyst carries a box warning that it may cause blood clots and is prohibited for pregnant women because it may lead to serious and life-threatening birth defects.
2. Prostate cancer drug-XOFIGO (radium dichloride)
May 2065438+03 15 US FDA gave priority to Bayer's advanced prostate cancer treatment drug Xofigo (radium dichloride) injection, three months ahead of schedule. The active ingredient of Xofigo is radium dichloride 223, which can emit alpha particles and has anticancer effect on bone metastatic cancer. The approval of Xofigo is based on a single clinical trial of 809 male androgen-resistant prostate cancer patients, who have spread to bones but not to other organs. The median survival time of male patients treated with Xofigo was 14 months, and that of male patients treated with placebo was 1 1.2 months. The most common adverse reactions of patients in Xofigo treatment group were nausea, diarrhea, vomiting and peripheral edema.
3. Drugs for metastatic melanoma
20 13 On May 29th, the FDA of the United States approved the listing of two metastatic melanoma drugs of GlaxoSmithKline, namely Tafinlar(Dabrafenib) and Mekinist (tramatinib).
Tafinlar is a BRAF kinase inhibitor, which is approved for the treatment of melanoma patients whose tumors express BRAFV600E gene mutation. BRAF is a serine/threonine protein kinase activated by guanosine binding protein RAS, which plays an important role in regulating mitogen-activated protein kinase (MAPK) signal pathway, and can normally regulate cell growth, division and differentiation, and can also cause cancer by forming carcinogenic mutants of RAF family members. The generation of BRAF V600 mutant significantly enhanced the activity of BRAF, which led to uncontrolled division of cancer cells. About 60% metastatic melanoma carries BRAF V600 mutant. Therefore, targeted inhibition of signal transduction of this carcinogenic mutant may be an effective method to treat melanoma.
Mekinist is a MEK kinase inhibitor, which has been approved for the treatment of melanoma patients whose tumors express BRAFV600E or V600K gene mutation. MEK is a rare bispecific kinase, which phosphorylates tyrosine and threonine to activate ERK. A large number of studies have shown that MEK inhibitors can inhibit the activation of ERK and block this pathway, thus achieving anti-tumor effects.
Third, contrast agent.
March 20th13rd13rd, FDA of the United States approved NAVIDEA's lymphatic mapping developer Lymphoek (Technetium TC-99m Tilmanocept). Lymphatic search injection is used in lymphatic mapping procedure to help locate the draining lymph nodes in patients with primary breast cancer/melanoma. Lymphoseek is the receptor of radiopharmaceuticals, which aims to identify and determine the one with the highest probability of canceration among many lymph nodes, thus helping doctors to stage patients' cancer.
On March 20th, 20 13, the FDA of the United States approved GUERBET's MRI contrast agent Dotarem (gadolinium meglumine acetate). Dotarem is a gadolinium-containing contrast agent, which has been approved for magnetic resonance imaging of brain (intracranial), spine and related tissues in adults and children (aged ≥2 years) to detect and display damaged blood-brain barrier and/or abnormal vascular distribution areas. Dotarem 0.5 mmol/ml contains 376.9 mg/ml gadolinium gluconate, which can be packed in glass bottles or pre-loaded syringes. The main adverse reactions of Dotarem include nausea, headache, pain or chills at the injection site and burning sensation.
Fourth, other drugs.
1. Hypercholesterolemia
201365438+1On October 29th, the FDA of the United States approved Kynamro (Mibomeisen sodium) produced by Jianzan Company for treating homozygous familial hypercholesterolemia as a lipid-lowering drug and dietary adjuvant drug to reduce low-density lipoprotein cholesterol, apolipoprotein B, total cholesterol and low-density lipoprotein cholesterol. Mibomeisen is the active component of Kynamro, which is an antisense oligonucleotide targeting human apolipoprotein B-100 messenger RNA. Apolipoprotein B-100 is the main apolipoprotein of low density lipoprotein and its metabolic precursor, very low density lipoprotein. Kynamro is another drug used to treat this hereditary cholesterol metabolic disorder after the FDA approved Juxtapid in February 20 12. The advantage of Kynamro is that the possibility of drug interaction is very small, because its metabolism does not affect the cytochrome P450 pathway involved in the metabolism of commonly used prescription drugs. Usage: subcutaneous injection of 200 mg per week 1 time. The FDA requires four studies after the drug goes on the market: the sensitivity analysis of the drug to double-stranded DNA; Evaluation of whether there is double-stranded DNA antibody in patients taking drugs: long-term registration of patients to determine the safety of drugs; Strengthen pharmacovigilance, monitor the reports of malignant tumor, immune-mediated reaction and liver abnormality of drug users.
2. An analgesic for menopausal women during sexual intercourse-Ospin.
20 13 On February 26th, the US FDA approved Shionogi's drug Osphena (ospemifene) for menopausal women's sexual pain. Oxopine is a new selective estrogen receptor modulator, which is used to treat female patients with moderate and severe sexual intercourse difficulty, so as to alleviate vulvar and vagina atrophy caused by the decrease of menopausal hormone level in some women. The medicine is taken daily 1 time, each time 1 tablet, which acts like a hormone in vaginal tissue, making vaginal tissue thicker and less fragile, and reducing the frequency of female sexual pain. Aspirin sodium has a black box warning on the label, pay attention to endometrial cancer and cardiovascular disease. FDA suggested that it has been proved that ospin can stimulate endometrium, cause endometrial thickening, and cause endometrial cancer because of its similar effect on vaginal tissue. FDA suggested that Osphena should prescribe the shortest treatment time; The black box warning also pointed out the incidence of thrombosis and hemorrhagic stroke (0.72‰ and 1.45‰ respectively) and the incidence of deep vein thrombosis (1.45‰).
3. A drug for chronic obstructive pulmonary disease-BREO ELIPTA (fluticasone furoate/Willant inhalation powder aerosol).
2013 may 10 FDA approves GlaxoSmithKline's drug Breo Ellipta for chronic obstructive pulmonary disease. The medicine is the inhalation compound powder of fluticasone furoate and Villandero, which is inhaled once a day. Fluticasone furoate in Breo Ellipta is an inhaled glucocorticoid, and wielandt is a long-acting β2 adrenoceptor agonist. The safety and efficacy of the drug were evaluated by a clinical trial involving 7700 patients with chronic obstructive pulmonary disease. Compared with the placebo group, the lung function of patients in the drug treatment group was improved and the number of disease attacks was reduced. When Breo Ellipta was approved, there was a black box warning in its label, suggesting that long-acting β2 adrenoceptor agonists could increase the risk of asthma-related death. The most common side effects reported by patients taking Breo Ellipta are nasal inflammation (nasopharyngitis), upper respiratory tract infection, headache and oral candidiasis (thrush).