380917-97-5
Name | PeraMpanel |
CAS | 380917-97-5 |
EINECS(EC#) | 691-969-4 |
Molecular Formula | C23H15N3O |
MDL Number | MFCD19443693 |
Molecular Weight | 349.385 |
MOL File | 380917-97-5.mol |
Synonyms
E 2007
CS-1116
Perampane
PeraMpanel
Pyronoprene
ER 155055-90
PeraMpanel-D5
PERAMPANEL API
PeraMpanel-13C6
Perampanel(E2007)
Perampanel Impurity
Perampanel Impurity 8
ER 155055-90 Perampanel
E 2007; ER 155055-90; E-2007; E2007
2-(2-oxo-1-phenyl-5-pyridin-2-
ylpyridin-3-yl)benzonitrile
Benzonitrile, 2-(1',6'-dihydro-6'-oxo-1'-phenyl[2,3'-bipyrid...
3-(2-Cyanophenyl)-1-phenyl-5-(2-pyridyl)-1,2-dihydropyridin-2-one
3-(2-Cyanophenyl)-5-(2-pyridyl)-1-phenyl-1,2-dihydropyridin-2-one
2-(6'-Oxo-1'-phenyl-1',6'-dihydro-[2,3'-bipyridin]-5'-yl)benzonitrile
Benzonitrile, 2-(1',6'-dihydro-6'-oxo-1'-phenyl[2,3'-bipyridin]-5'-yl)-
2-(2-oxo-1-phenyl-5-(pyridin-2-yl)-1,2-dihydropyridin-3-yl)benzonitrile
Perampanel/D3-labelled (3R,4R)-1-Benzyl-N,4-dimethylpiperidine-3-amine dihydrochloride
Perampane,Perampanel
Benzonitrile, 2-(1',6'-dihydro-6'-oxo-1'-phenyl[2,3'-bipyridin]-5'-yl)
Chemical Properties
Boiling point | 619.1±55.0 °C(Predicted) |
density | 1.31±0.1 g/cm3(Predicted) |
solubility | Soluble in DMSO |
form | Powder |
pka | 4.73±0.19(Predicted) |
Hazard Information
Definition
ChEBI: A member of the class of bipyridines that is 2,3'-bipyridin-6'-one substituted at positions 1' and 5' by phenyl and 2-cyanophenyl groups respectively. Used as an adjunctive therapy for the treatment of partial-onset seizures in patients with epilepsy.
Originator
Eisai (Japan)
Uses
Isotope labelled Perampanel (P285520), is an antiepileptic drug. It inhibits α-amino-3-hydroxy-5-methyl-4-isoxazole-propionic acid (AMPA)-induced increases in intracellular Ca2+ and selectively blocks AMPA receptor-mediated synaptic transmission, thus reducing neuronal excitation.
Brand name
Fycompa
Clinical Use
Selective AMPA-type glutamate receptor antagonist:
Antiepileptic
Antiepileptic
Drug interactions
Potentially hazardous interactions with other drugs
Antidepressants: anticonvulsant effect antagonised; avoid with St John’s wort.
Antiepileptics: concentration reduced by carbamazepine, fosphenytoin, oxcarbazepine and phenytoin.
Antimalarials: anticonvulsant effect antagonised by mefloquine.
Antipsychotics: anticonvulsant effect antagonised.
Orlistat: possibly increased risk of convulsions.
Progestogens: high-dose perampanel reduces plasma concentration of progestogens (possibly reduced contraceptive effect).
Antidepressants: anticonvulsant effect antagonised; avoid with St John’s wort.
Antiepileptics: concentration reduced by carbamazepine, fosphenytoin, oxcarbazepine and phenytoin.
Antimalarials: anticonvulsant effect antagonised by mefloquine.
Antipsychotics: anticonvulsant effect antagonised.
Orlistat: possibly increased risk of convulsions.
Progestogens: high-dose perampanel reduces plasma concentration of progestogens (possibly reduced contraceptive effect).
Metabolism
Extensively metabolised via primary oxidation via the
cytochrome P450 isoenzyme CYP3A sub family and
sequential glucuronidation.
Perampanel is excreted in the urine and faeces mainly as oxidative and conjugated metabolites.
Perampanel is excreted in the urine and faeces mainly as oxidative and conjugated metabolites.
Questions And Answer
-
Description
Perampanel (licensed in 2012) is a third- generation AED known with the proprietary brand name of Fycompa® (Eisai, Hatfield) in the UK and Banzel® (Eisai, Hatfield) in the USA. ; -
Indications
Epilepsy: Adjunctive treatment of focal seizures with or without secondary generalization and primary generalized tonic- clonic seizures. ; -
Dose titration
Epilepsy— adjunctive therapy: 2 mg nocte for at least 14 days, then increased by 2 mg every 14 or more days; usual maintenance 4– 8 mg nocte (max. 12 mg nocte). ; -
Interactions
With AEDs- Some AEDs known as CYP450 3A enzyme inducers (carbamazepine, oxcarbazepine, phenytoin) have been shown to increase perampanel clearance and consequently to decrease plasma concentrations of perampanel. Carbamazepine, a known potent enzyme inducer, reduced perampanel levels by two- thirds in a study performed on healthy subjects
- In the epilepsy population pharmacokinetic analysis, perampanel was found to decrease the clearance of oxcarbazepine by 26%. Oxcarbazepine is rapidly metabolized by cytosolic reductase enzyme to the active metabolite, monohydroxycarbazepine. The effect of perampanel on monohydroxycarbazepine concentrations is not known.
With other drugs- Strong inducers of cytochrome P450, such as rifampicin and St John’s Wort (Hypericum perforatum), are expected to decrease perampanel concentrations.
- In healthy subjects, the CYP3A4 inhibitor ketoconazole increases perampanel exposure.
- Perampanel can make certain hormonal contraceptives such as levonorgestrel less effective.
- Decrease in exposure of midazolam may be caused by perampanel.
With alcohol/food- Drinking alcohol while taking perampanel can affect a patients’ alertness and ability to drive or use tools or machines. It can also aggravate irritability, confusion, and depression.
- There are no specific foods that must be excluded from diet when taking perampanel.
-
Special populations
Hepatic impairment- Increase at intervals of at least 2 weeks, up to a maximum of 8 mg daily, in mild- to- moderate impairment.
- Avoid in severe impairment.
Renal impairment
Avoid in moderate or severe impairment.
Pregnancy- There are limited amount of data available on the use of perampanel in pregnant women and the potential risk for humans is unknown.
- Perampanel is not recommended in pregnancy and female patients must use a reliable method of contraception to avoid becoming pregnant while being treated with perampanel (this should be continued for 1 month after stopping treatment).
- As perampanel can make certain hormonal contraceptives such as levonorgestrel less effective, other forms of safe and effective contraception (such as a condom or coil) should be used when taking perampanel (this should be continued for 1 month after stopping treatment).
- Perampanel has been found to be present in milk in animal studies and it is recommended that breastfeeding should be avoided.
-
Behavioural and cognitive effects in patients with epilepsy
For this third- generation agent, clinical experience is still limited, and little is known about its positive and negative psychotropic properties, and their implications for the management of behavioural symptoms in patients with epilepsy. There are initial reports of behavioural disturbances (especially depression, anxiety, irritability, and psychosis), which seem to be dose- related and tend to appear within the first weeks of treatment. Reports of cognitive effects (mainly affecting memory) are relatively rare. ; -
Psychiatric use
Perampanel has no indications for the treatment of psychiatric disorders. There is insufficient experience with perampanel to draw any conclusion regarding its psychotropic profile. ;
Supplier
Suzhou Zehou Biotechnology Co. , Ltd.
Telephone0512-68716880 18075373931
Website
Shanghai Boyle Chemical Co., Ltd.
Telephone
Websitehttp://www.boylechem.com
J & K SCIENTIFIC LTD.
Telephone010-82848833 400-666-7788
Websitehttp://www.jkchemical.com
Jia Xing Isenchem Co.,Ltd
Telephone0573-85285100 18627885956
Websitehttps://www.chemicalbook.com/ShowSupplierProductsList14265/0.htm
Chemsky(shanghai)International Co.,Ltd.
Telephone021-50135380
Websitehttp://www.shchemsky.com
Wuhan Fortuna Chemical Co., Ltd
Telephone027-027-59207852 13308628970
Websitehttp://www.fortunachem.cn
S.Z. PhyStandard Bio-Tech. Co., Ltd.
Telephone0755-83725681-603
Websitehttp://www.phystandard.com.cn
Shanghai Witofly Chemical Co.,Ltd
Telephone
Websitehttp://www.witofly.com
AstaTech (Chengdu) Pharma. Co., Ltd.
Telephone15928766785 15928766785
Websitehttp://www.astabiochem.cn/
Nanjing Sunlida Biological Technology Co., Ltd.
Telephone025-57798810
Websitehttp://www.sunlidabio.com
Cato Research Chemicals Inc.
Telephone020-81960175
Websitehttp://www.cato-chem.com
ShangHai Caerulum Pharma Discovery Co., Ltd.
Telephone 18149758185
Websitehttp://www.caerulumpharma.com
Suzhou yacoo science co.,Ltd
Telephone0512-87182056 18013166090
Websitehttp://www.yacoo.com.cn
NINGBO INNO PHARMCHEM CO.,LTD.
Telephone86-574-27787657
Websitehttp://www.dearchem.com
Shanghai YuLue Chemical Co., Ltd.
Telephone021-60345187 13671753212
Websitehttps://www.chemicalbook.com/ShowSupplierProductsList16365/0.htm
Shanghai Kewel Chemical Co., Ltd.
Telephone021-64609169 18901607656
Websitehttp://www.kewelchem.com/
Hangzhou J&H Chemical Co., Ltd.
Telephone+86-571-87396432
Websitehttp://www.jhechem.com
AdooQ Bioscience CHINA
Telephone025-58849295 18951903616;
Websitehttp://www.adooq.cn
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