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Use of 1,2,4-oxadiazole N-oxide-pyridine compounds and combinations with other drugs

IP.com Disclosure Number: IPCOM000220262D
Publication Date: 2012-Jul-27
Document File: 4 page(s) / 37K

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The IP.com Prior Art Database

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Page 01 of 4

BIA 9-1067 (2,5-dichloro-3-(5-(3,4-dihydroxy-5-nitrophenyl)-1,2,4-oxadiazol-3-yl)-4,6- dimethylpyridine 1-oxide), INN: opicapone, is a COMT inhibitor (COMTi) being developed to be used in Parkinson's Disease (PD) patients, restless legs syndrome patients or patients suffering from other movement disorders. BIA 9-1067 may also be used for the treatment of gastrointestinal disturbances, edema formation states and hypertension in patients suffering therefrom.

BIA 9-1067 may be administered (sequentially or simultaneously) with L-DOPA/DDCi, L- DOPA/DDCi/COMTi and/or DDCi preparations such as the shown in table 1 (see below). When administering simultaneously (e.g. concomittanlty) BIA 9-1067, L-DOPA and/or a DDCi, all drugs may be provided in a single dosage form, for example a capsule, tablet, powder, spray or a gel, which can be an immediate release, extended release or controlled release dosage form. Typically, BIA 9-1067 is administered from thrice daily to once weekly, for example, thrice daily, twice daily, once daily, once every other day, once every 3 days, once every 4 days, once every 5 days, once every 6 days or once every seven days. The total daily dosage of BIA 9-1067 ranges from 0.5 to 300 mg/daily, for example 0.5, 1, 2, 3, 4, 5, 10, 15, 20, 25, 30, 40, 50, 60, 70, 75, 80, 90, 100, 125, 150, 175, 200, 250 or 300 mg/daily. The administration of BIA 9-1067 may be made at any period of time of the day or night, for example the morning, midday, afternoon, evening or night, with or without food.

Table 1. Combination of BIA 9-1067 with L-DOPA/DDCi, L-DOPA/DDCi/COMTi and DDCi preparations.

Combinations with BIA 9-1067

Capsules/Tablets/Other

Dosage(s)

Administration

Immediate Release (IR) /

(mg/mg)

regime(s)

Controlled Release (CR)

L-DOPA/DDCi preparations

L-DOPA/Carbidopa

IR

50/12,5

400-1600mg of L-

100/10

DOPA and carbidopa

100/25

Orally Disintegrating

250/25

 100-650mg daily in divided doses (2 to 10 doses per day, for

example, 2, 3, 4, 5, 6,

7, 8, 9 or 10 doses a

day)

100/10

100/25

250/25

CR

200/50

100/25

Intestinal Gel

20/5

L-DOPA/Benserazide

Capsules/Tablets

50/12,5

400-1600mg of L-

100/25

DOPA and

200/50

Dispersible Tablets

50/12,5

  benserazide 100- 650mg daily in divided doses (2 to 10 doses

per day, for example,

2, 3, 4, 5, 6, 7, 8, 9 or

10 doses a day)

100/25

Controlled release

100/25

L-DOPA/DDCi/COMTi

Capsules/Tablets/Other

Dosage(s)

Administration

(mg/mg/mg)

regime(s)

L-DOPA/carbidopa/entacapone

50/12.5/200

150-1200mg of L-

(e.g. Stalevo®)

75/18.75/200

DOPA, carbidopa 100-

100/25/200

125/31.25/200

   650mg and entacapone 600-2000 mg daily in divided

doses (2 to 10 doses

per day, for example,

2, 3, 4, 5, 6, 7, 8, 9 or

10 doses a day)

150/37.5/200

200/50/200


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DDCi

Capsules/Tablets/Other

Dosage(s) (mg)

Administration

regime(s)

Carbidopa (e.g. Lodosyn®)

IR or CR

25


12.5

 Carbidopa may be used simultaneously or sequentially with any

of the available L-

DOPA/DDCi or L-

 DOPA/DDCi/COMTi preparations, together with...