Nalfurafine Hydrochloride

Nalfurafine hydrochloride was approved by Pharmaceuticals and Medical Devices Agency of Japan (PMDA) on Jan 21, 2009. It was developed and marketed as Remitch® by Toray and Torii on Mar 24, 2009 in Japan.

Nalfurafine hydrochloride is a κ-opioid receptor agonist to suppress itch. It controls itch when other existing antihistamine or antiallergic drugs are ineffectual. It is indicated for improvement of itch in hemodialysis when other existing treatment is insufficient.

Remitch® is available as capsule for oral use, containing 2.5 μg of Nalfurafine hydrochloride. The recommended dose is 1 capsule (2.5 μg) once daily after supper for adults.

Index：

General Information

Update Date：2016-05-16

Drug Name：
Nalfurafine Hydrochloride
Research Code：
AC-820; TRK-820
Trade Name：
Remitch®
MOA：
κ-opioid receptor agonist
Indication：
Uremic pruritus
Status：
Approved
Company：
Toray (Originator) , Torii
Sales：
$129.6 Million (Y2015);
$114.7 Million (Y2014);
$145.9 Million (Y2013);
$128.7 Million (Y2012);
$118.4 Million (Y2011);
ATC Code：
V03AX02
Approved Countries or Area

Update Date：2015-08-27

Approval Date Approval Type Trade Name Indication Dosage Form Strength Company Review Classification
2009-01-21 Marketing approval Remitch Uremic pruritus Capsule 2.5 μg Nalfurafine Hydrochloride Toray, Torii
More
Chemical Structure

Update Date：2015-08-27

Molecular Weight 513.03
Formula C28H32N2O5 • HCl
CAS No. 152657-84-6 (Nalfurafine );
152658-17-8 (Nalfurafine HCl);
Chemical Name (2E)-N-[(5R,6R)-17-(Cyclopropylmethyl)-4, 5-epoxy-3, 14-dihydroxymorphinan-6-yl]-3-(furan-3-yl)-N-methylprop-2-enamide monohydrochloride
Nalfurafine （Free Acid/Base）Parameters：
MW HD HA FRB* PSA* cLogP*
476.56 2 7 7 86.4 1.808±0.597
*：Calculated by ACD/Labs software V11.02.
Related Patents

Update Date：2015-11-17

No. Major Technical Classification Publication No. Patent No. Legal Status Filling Date Estimated Expiry Date
1 Formula CN1111900A Withdrawn 1994/6/28
2 Uses CN1214634A CN1180844C Granted 1997/11/21 2017/11/21
3 Others CN1530111A CN1291717C Granted 1997/11/21 2017/11/21
4 Uses CN1535687A Refusal 1997/11/21
5 Uses CN1382145A CN1204139C Granted 2000/8/24 2020/8/24
6 Uses CN1537016A CN100398154C Granted 2002/3/29 2022/3/29
7 Uses CN1507356A CN1283317C Granted 2002/5/8 2022/5/8
8 Uses CN101137658A CN101137658B Granted 2006/3/9 2026/3/9
9 Crystal CN101155814A CN101155814B Granted 2006/4/6 2026/4/6
10 Uses CN101686977A CN101686977B Granted 2008/4/24 2028/4/24
11 Uses CN101778632A CN101778632B Granted 2008/6/20 2028/6/20
12 Uses CN101848714A CN101848714B Granted 2008/10/3 2028/10/3
13 Formulation CN102196811A CN102196811B Granted 2009/10/23 2029/10/23
14 Formulation CN102448445A CN102448445B Granted 2010/3/29 2030/3/29
15 Uses CN102711759A CN102711759B Granted 2011/1/28 2031/1/28
16 Uses CN103327977A Examination 2012/1/30
More
Synthesis & Impurities

Update Date：2015-12-25


1. WO9315081A1 / US6323212B1. 

2. WO9501178A1 / US5739145A.

3. US6177438B1.

4. WO2010144641A1 / US2010317683A1.

 

Impurity database is being updated！