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Japanese filing for Amgen’s PCSK9 inhibitor Repatha
Amgen has filed its closely watched PCSK9 inhibitor Repatha (evolocumab) in Japan for the treatment of high cholesterol.
Repatha is an investigational fully human monoclonal antibody that inhibits proprotein convertase subtilisin/kexin type 9 (PCSK9), a protein that reduces the liver’s ability to remove low-density lipoprotein cholesterol (LDL-C), or ‘bad’ cholesterol, from the blood.
| Monoclonal antibody | |
|---|---|
| Type | Whole antibody |
| Source | Human |
| Target | PCSK9 |
| Clinical data | |
|
|
| Subcutaneous injection | |
| Identifiers | |
| 1256937-27-5 | |
| C10AX13 | |
| Chemical data | |
| Formula | C6242H9648N1668O1996S56 |
| 141.8 kDa | |
Evolocumab[1] (also known as compound number AMG-145 or AMG145)[2] is a monoclonal antibody designed for the treatment of hyperlipidemia.[3] Evolocumab is a fully human monoclonal antibody that inhibits proprotein convertase subtilisin/kexin type 9 (PCSK9).
PCSK9 is a protein that targets LDL receptors for degradation and thereby reduces the liver’s ability to remove LDL-C, or “bad” cholesterol, from the blood.
Evolocumab, being developed by Amgen scientists, is designed to bind to PCSK9 and inhibit PCSK9 from binding to LDL receptors on the liver surface. In the absence of PCSK9, there are more LDL receptors on the surface of the liver to remove LDL-C from the blood.
Clinical trials
Two trials have been in progress as at mid-2014:
On 23 January 2014 Amgen announced that the Phase 3 GAUSS-2 (Goal Achievement After Utilizing an Anti-PCSK9 Antibody in Statin Intolerant Subjects-2) trial evaluating evolocumab in patients with high cholesterol who cannot tolerate statins met its co-primary endpoints: the percent reduction from baseline in low-density lipoprotein cholesterol (LDL-C) at week 12 and the mean percent reduction from baseline in LDL-C at weeks 10 and 12. The mean percent reductions in LDL-C, or “bad” cholesterol, compared to ezetimibe were consistent with results observed in the Phase 2 GAUSS study.[4][5]
The GAUSS-2 trial evaluated safety, tolerability and efficacy of evolocumab in 307 patients with high cholesterol who could not tolerate effective doses of at least two different statins due to muscle-related side effects. Patients were randomly assigned to one of four treatment groups: subcutaneous evolocumab 140 mg every two weeks and oral placebo daily; subcutaneous evolocumab 420 mg monthly and oral placebo daily; subcutaneous placebo every two weeks and oral ezetimibe 10 mg daily; or subcutaneous placebo monthly and oral ezetimibe 10 mg daily.
Safety was generally balanced across treatment groups. The most common adverse events (> 5 percent in evolocumab combined group) were headache (7.8 percent evolocumab; 8.8 percent ezetimibe), myalgia (7.8 percent evolocumab; 17.6 percent ezetimibe), pain in extremity (6.8 percent evolocumab; 1.0 percent ezetimibe), and muscle spasms (6.3 percent evolocumab; 3.9 percent ezetimibe).
Cholesterol-lowering treatment with a statin as part of follow-up care can help reduce a patient’s risk after myocardial infarction, ischaemic stroke or TIA.
The FOURIER Phase 3 clinical study http://www.fourierstudy.com/ seeks to find out whether lowering cholesterol by an additional 50% might reduce this risk even further. Several sites in the UK are part of this very large clinical study, lasting up to five years, and it is hoped that the study will help guide future clinical practice.
Evolocumab (also formerly known as AMG145, from Amgen) binds to PCSK9, a natural protein produced by the liver. By binding to PCSK9, evolocumab allows the LDL receptor (a protein present in the liver) to move LDL-cholesterol out of the bloodstream more efficiently. This study is designed to see whether treatment of dyslipidemia with evolocumab in people who have experienced a prior myocardial infarction, ischaemic stroke or TIA, and who are taking a highly effective dose of a statin, reduces the risk of recurring or additional cardiovascular events. Participants in this study have clinically evident cardiovascular disease.
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References
- World Health Organization (2012). “International Nonproprietary Names for Pharmaceutical Substances (INN). Proposed INN: List 108” (PDF). WHO Drug Information 26 (4).
- 2
- Sheridan, C (2013). “Phase 3 data for PCSK9 inhibitor wows”. Nature Biotechnology 31 (12): 1057–8. doi:10.1038/nbt1213-1057. PMID 24316621.
- 3
- Statement On A Nonproprietary Name Adopted By The USAN Council – Evolocumab
- 4
- Estel Grace Masangkay, “Amgen Phase III GAUSS-2 Trial of Evolocumab (AMG 145) Meets Co-Primary Endpoints Of LDL Cholesterol Reduction”, Bioresearch Online (January 24 2014)
- 5
Pierson, Ransdell (17 March 2014). “Amgen drug meets goal for those with high genetic cholesterol”. Associated Press. Retrieved 19 March 2014.
ONO Pharmaceutcal files for approval of Additional Indication for Onoact® 50 injection, Short-Acting Selective β1 Blocker in Japan
disease. AF/AFL with LV dysfunction accompanying by persistent elevated heart rate would lead to further deterioration of cardiac performance. Swift rate control is inevitable to be restored from this detrimental condition, however, no drug on market can provide both the features of fast-acting and easy titratability for tachyarrhythmia (AF/AFL) with LV dysfunction.
Onoact® 50 for injection is the short-acting selective β1 blocker which reduces heart rate by selectively blocking β1 receptors located chiefly in the heart and this fast-acting drug can be easily titrated.
We expect that Onoact® 50 for injection can contribute to promptly reducing heart rate without causing deterioration of cardiac performance in treatment of tachyarrhythmia (AF/AFL) with LV dysfunction.
This short-acting selective β1 blocker drug is discovered and developed by ONO and has been widely used by many patients since its launch. The drug has firstly received approval for emergency treatment of intra-operative tachyarrhythmia (atrial fibrillation and flutter, and sinus tachycardia) in July 2002. Then, it had also been approved for additional indication of emergency treatment of post-operative tachyarrhythmia (atrial fibrillation and flutter, and sinus tachycardia) with monitoring of circulatory dynamics in October 2006.
| Identifiers | |
|---|---|
| CAS number | 133242-30-5 |
| Chemical data | |
| Formula | C25H39N3O8 |
| Mol. mass | 509.59 g/mol |
Landiolol (INN) is a drug which acts as a highly cardioselective, ultra short-acting beta blocker. It is used as an anti-arrhythmic agent.
- Yoshiya I (December 1998). “[Landiolol hydrochloride, a new sympathetic beta blocker]” (in Japanese). Masui 47 Suppl: S126–32. PMID 9921175.
- Ogata J, Okamoto T, Minami K (2003). “Landiolol for the treatment of tachyarrhythmia associated with atrial fibrillation”. Can J Anaesth 50 (7): 753. doi:10.1007/BF03018726. PMID 12944459
Chugai files Herceptin for post surgical Adjuvant treatment of HER2+ve breast cancer in Japan
Trastuzumab, monoclonal antibody
Thursday, 7 February 2013
Trastuzumab (INN; trade names Herclon, Herceptin) is a monoclonal antibody that interferes with the HER2/neu receptor. Its main use is to treat certain breast cancers.
The HER receptors are proteins that are embedded in the cell membrane and communicate molecular signals from outside the cell (molecules called EGFs) to inside the cell, and turn genes on and off. The HER proteins stimulate cell proliferation. In some cancers, notably certain types of breast cancer, HER2 is over-expressed, and causes cancer cells to reproduce uncontrollably.[1]
The original studies of trastuzumab showed that it improved overall survival in late-stage (metastatic) breast cancer from 20.3 to 25.1 months,[1] but there is controversy over whether trastuzumab is effective in earlier stage cancer.[2]Trastuzumab is also controversial because of its cost, as much as $100,000 per year,[3] and while certain private insurance companies in the U.S. and government health care systems in Canada, England and elsewhere have refused to pay for trastuzumab for certain patients, some companies have since accepted trastuzumab treatment as a covered preventative treatment.[4]
Trastuzumab is also being studied for the treatment of other cancers.[5] It has been used with some success in women with uterine papillary serous carcinomas that overexpress HER2/neu.[6]
References
- Hudis, CA (2007). “Trastuzumab–mechanism of action and use in clinical practice”. N Engl J Med. 357 (1): 39–51.doi:10.1056/NEJMra043186. PMID 17611206. Jul 5;357(1):39-51. Review /article
- 129 Herceptin and early breast cancer: a moment for caution [Editorial]. Lancet 2005;366:1673.
- “Herceptin or Trastuzumab: Efficacy, Side Effects”. Health and Life.
- “At last, Axa pays for Herceptin”. 2006.
- Vecchione L. Novel investigational drugs for gastric cancer.Expert Opin Investig Drugs. 2009 May 26. [Epub ahead of publication]. Review /article.
- Santin AD, Bellone S, Roman JJ, McKenney JK, Pecorelli S. (2008). “Trastuzumab treatment in patients with advanced or recurrent endometrial carcinoma overexpressing HER2/neu”.Int J Gynaecol Obstet 102 (2): 128–31.doi:10.1016/j.ijgo.2008.04.008. PMID 18555254.
New Drug Approvals 
