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Phase 2 SMP-986(afacifenacin fumarate) Overactive bladder/ Dainippon Sumitomo Pharma and Nippon Shinyaku conclude a license agreement for SMP-986, a therapeutic agent for urology
877606-63-8 cas no of afacifenacin
any str error, mail to amcrasto@gmail.com
SMP-986 (afacifenacin fumarate)
(4S)-4-phenyl-3-(1-{[3-(trifluoromethoxy)phenyl]methyl}piperidin- 4-yl)-3,4-dihydroquinazolin-2(1H)-one muscarinic receptor antagonist

- Developed in-house
- SMP-986 possesses the dual pharmacological actions of muscarinic receptor antagonism (non-selective) and inhibition of the bladder afferent pathway through Na+-channel blockade. This compound is being evaluated for its ability to ease urinary urgency and reduce the frequency of both urination and incontinence. The compound has also exhibited the potential to have lower incidence of side effects related to muscarinic receptor antagonism, such as dry mouth.
- Development stage: Phase II in the U.S. and Europe. Phase II in Japan
7 mar 2013
Dainippon Sumitomo Pharma Co., Ltd. (DSP) and Nippon Shinyaku Co., Ltd. Announce they have concluded a license agreement for exclusive rights to develop, manufacture and commercialize SMP-986 in Japan, a new therapeutic agent for overactive bladder created by DSP.
Taiho Pharma seeks Japanese nod to manufacture,market novel anti-tumour agent TAS-102
TRIFLURIDINE

TIPIRACIL
TAS-102 is an anti-cancer drug under development for colorectal cancer.[1]
| Combination of | |
|---|---|
| Trifluridine | cytotoxin |
| Tipiracil | thymidine phosphorylase inhibitor |
Clinical trials
A phase II trial reported in 2011[2] and a phase III trial is due to end in 2014.[1][3]
Mechanism
TAS-102 consists of the cytotoxin trifluridine and the thymidine phosphorylase inhibitor (TPI) tipiracil.[4] Trifluridine is incorporated into DNA during DNA synthesis and inhibits tumor cell growth. Tipiracil protects trifluridine from being broken down when taken orally.
| February 28, 2013, |
|
Taiho Pharmaceutical Co., Ltd. has submitted an application to the Japanese Ministry of Health, Labour and Welfare for approval of the manufacture and marketing of the novel oral nucleoside anti-tumour agent TAS-102 (combination of trifluorothymidine [FTD] and tipiracil hydrochloride [TPI]). Taiho is seeking approval of TAS-102 for the indication of unresectable, advanced, recurrent colorectal cancer. The application for approval is based on the results of a phase II clinical trial (Study 10040030) conducted at 20 facilities throughout Japan. It was a randomized, double-blind comparative study of TAS-102 and a placebo involving 172 patients with unresectable, advanced, recurrent colorectal cancer that was refractory to the standard chemotherapy of at least two or more regimens containing fluoropyrimidine, irinotecan, and oxaliplatin. The results indicated that the group administered TAS-102 had improved overall survival rates (median overall survival: 9.0 months vs. 6.6 months) and a significantly reduced risk of mortality (HR: 0.56, p=0.0011). The most frequently reported adverse drug reaction with a CTCAE grade of 3 or higher was neutropenia. Grade 3 or higher diarrhea, fatigue, nausea, and other adverse reactions were no more than 10 per cent. Taiho Pharmaceutical is currently proceeding with a global phase III clinical trial of TAS-102 in a similar colorectal cancer population (RECOURSE) with the ultimate goal of global registration and commercialization of the agent. Taiho Pharmaceutical believes that TAS-102 will make a significant contribution to cancer patients and will continue its development efforts to broaden its use. TAS-102 is an anti-tumour agent composed of a combination of trifluorothymidine (FTD), a nucleoside that incorporates into DNA and inhibits a variety of genetic functions required for the proliferation of cancer cells, and tipiracil hydrochloride (TPI), an inhibitor of thymidine phosphorylase (which degrades FTD) that maintains an effective blood concentration of FTD. TAS-102 is administered twice daily to achieve a total daily dose of 70mg/m2 for five days followed by two days of rest and then repeated a second time. This is followed by a 14-day rest period to make a 28-day schedule for one course. |
- “New Drug for Colorectal Cancer Shows Promise in Phase II Trial”. 28 Aug 2012.
- “Novel Drug TAS-102 Makes Headway in Refractory Colorectal Cancer”. 4 Oct 2011.
- “Phase II study of TAS-102 for pretreated metastatic colorectal cancer”. 29 Aug 2012.
- “A novel combination antimetabolite, TAS-102, exhibits antitumor activity in FU-resistant human cancer cells through a mechanism involving FTD incorporation in DNA.”. Sept 2004.
| TRIFLURIDINE | |
|---|---|
| 1-[4-hydroxy-5-(hydroxymethyl)oxolan-2-yl]-5- (trifluoromethyl) pyrimidine-2,4-dione |
Trifluridine (also called trifluorothymidine or TFT) is an anti-herpesvirus antiviral drug, used primarily on the eye. It was sold under the trade name, Viroptic, by Glaxo Wellcome, now merged into GlaxoSmithKline. The brand is now owned by Monarch Pharmaceuticals, which is wholly owned by King Pharmaceuticals.
It is a nucleoside analogue, a modified form of deoxyuridine, similar enough to be incorporated into viral DNA replication, but the -CF3 group added to the uracil component blocks base pairing.
It is a component of the experimental anti-cancer drug TAS-102.
TIPIRACIL
| NAME | 5-chloro-6-[(2-iminopyrrolidin-1-yl)methyl]pyrimidine-2,4-(1H,3H)-dione | |||
| CAS | 183204-74-2 | |||
| MOL F | C9H11ClN4O2 | |||
| STR | ![]() |
|||
| USE | potentiator of antineoplastics; | |||
Taiho Pharmaceutical, a subsidiary of Otsuka Holdings Co., Ltd., is an R&D-driven specialty pharma focusing on the three fields of oncology, allergies and immunology, and urology.
DRUG APPROVALS BY DR ANTHONY MELVIN CRASTO
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