NZ758246B2 - Dosing regimen for missed doses for long-acting injectable paliperidone esters - Google Patents
Dosing regimen for missed doses for long-acting injectable paliperidone esters Download PDFInfo
- Publication number
- NZ758246B2 NZ758246B2 NZ758246A NZ75824616A NZ758246B2 NZ 758246 B2 NZ758246 B2 NZ 758246B2 NZ 758246 A NZ758246 A NZ 758246A NZ 75824616 A NZ75824616 A NZ 75824616A NZ 758246 B2 NZ758246 B2 NZ 758246B2
- Authority
- NZ
- New Zealand
- Prior art keywords
- paliperidone palmitate
- dose
- reinitiation
- administered
- injectable paliperidone
- Prior art date
Links
- PMXMIIMHBWHSKN-UHFFFAOYSA-N 3-{2-[4-(6-fluoro-1,2-benzoxazol-3-yl)piperidin-1-yl]ethyl}-9-hydroxy-2-methyl-6,7,8,9-tetrahydropyrido[1,2-a]pyrimidin-4-one Chemical class FC1=CC=C2C(C3CCN(CC3)CCC=3C(=O)N4CCCC(O)C4=NC=3C)=NOC2=C1 PMXMIIMHBWHSKN-UHFFFAOYSA-N 0.000 title 1
- VOMKSBFLAZZBOW-UHFFFAOYSA-N 3-{2-[4-(6-fluoro-1,2-benzoxazol-3-yl)piperidin-1-yl]ethyl}-2-methyl-4-oxo-6,7,8,9-tetrahydropyrido[1,2-a]pyrimidin-9-yl hexadecanoate Chemical compound FC1=CC=C2C(C3CCN(CC3)CCC3=C(C)N=C4N(C3=O)CCCC4OC(=O)CCCCCCCCCCCCCCC)=NOC2=C1 VOMKSBFLAZZBOW-UHFFFAOYSA-N 0.000 claims abstract 43
- 229960000635 paliperidone palmitate Drugs 0.000 claims abstract 40
- 238000002347 injection Methods 0.000 claims 8
- 239000007924 injection Substances 0.000 claims 8
- 210000000852 deltoid muscle Anatomy 0.000 claims 6
- 239000003814 drug Substances 0.000 claims 6
- 208000020925 Bipolar disease Diseases 0.000 claims 4
- 101150013568 US16 gene Proteins 0.000 claims 4
- 210000003205 muscle Anatomy 0.000 claims 4
- 201000000980 schizophrenia Diseases 0.000 claims 4
- 208000028017 Psychotic disease Diseases 0.000 claims 3
- 238000004519 manufacturing process Methods 0.000 claims 2
- 239000002245 particle Substances 0.000 claims 2
- 239000000725 suspension Substances 0.000 claims 2
- 239000008365 aqueous carrier Substances 0.000 claims 1
- 230000000977 initiatory effect Effects 0.000 claims 1
- 238000009472 formulation Methods 0.000 abstract 2
- 239000000203 mixture Substances 0.000 abstract 2
- 238000000034 method Methods 0.000 abstract 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/02—Inorganic compounds
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
- A61K47/12—Carboxylic acids; Salts or anhydrides thereof
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K47/26—Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
- A61K47/34—Macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyesters, polyamino acids, polysiloxanes, polyphosphazines, copolymers of polyalkylene glycol or poloxamers
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
- A61K9/0024—Solid, semi-solid or solidifying implants, which are implanted or injected in body tissue
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/10—Dispersions; Emulsions
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/24—Antidepressants
Abstract
The present application provides a method for treating patients in need of psychiatric treatment, wherein said patient is being treated with the 3-month formulation of paliperidone palmitate and fails to take the next scheduled dose of the 3-month formulation of paliperidone palmitate.
Claims (10)
1. A use of paliperidone palmitate in the manufacture of a medicament for use in treating a patient in need of psychiatric treatment for psychosis, schizophrenia, or bipolar disorder 5 that has been treated with a 3-month injectable paliperidone palmitate depot, wherein between greater than or equal to 4 months and up to and including 9 months have elapsed since the last injection of the 3-month injectable paliperidone palmitate depot, wherein said medicament is a 3-month injectable paliperidone palmitate depot (PP3M), and wherein said medicament is to be used in a dosing regimen comprising: 10 (1) a first reinitiation loading dose of a monthly injectable paliperidone palmitate depot to be administered intramuscularly in the deltoid muscle of said patient; (2) a second reinitiation loading dose of the monthly injectable paliperidone palmitate depot to be administered in the deltoid muscle of said patient on about the 4th day to about the 12th day after administering said first reinitiation loading dose; and 15 (3) a reinitiation dose of the 3-month injectable paliperidone palmitate depot in the range of about 175mg eq. to about 525 mg eq. to be administered in the deltoid or gluteal muscle of said patient on about the 23rd day to about the 37th day after administering the second reinitiation loading dose of monthly injectable paliperidone palmitate, 20 wherein said first and second reinitiation loading dose and the reinitiation dose of the 3- month injectable paliperidone palmitate depot are selected from the table below based on the dose administered at the last injection of the 3-month injectable paliperidone palmitate depot Dose PP1M to be administered, two doses PP3M to be administered administered (into deltoid muscle) (into deltoid or gluteal muscle) at last injection of First Second Reinitiation Dose Reinitiation Dose Reinitiation Dose 175 mg eq. 50 mg eq. 50 mg eq. 175 mg eq. 263 mg eq. 75 mg eq. 75 mg eq. 263 mg eq. 350 mg eq. 100 mg eq. 100 mg eq. 350 mg eq. 525 mg eq. 100 mg eq. 100 mg eq. 525 mg eq. wherein the 3-month injectable paliperidone palmitate depot is a suspension of paliperidone palmitate having an average particle size of less than 20 µm to 3 µm; 5 wherein no intervening doses of paliperidone palmitate have been administered in between the last injection of the 3-month injectable paliperidone palmitate depot and the first reinitiation loading dose.
2. A use of paliperidone palmitate in the manufacture of a medicament for use in 10 treating a patient in need of psychiatric treatment for psychosis, schizophrenia, or bipolar disorder that has been treated with a 3-month injectable paliperidone palmitate depot, wherein between greater than or equal to 4 months and up to and including 9 months have elapsed since the last injection of the 3-month injectable paliperidone palmitate depot, wherein said medicament is a 1-month injectable paliperidone palmitate depot (PP1M), 15 and wherein said medicament is to be used in a dosing regimen comprising: (1) a first reinitiation loading dose of a monthly injectable paliperidone palmitate depot to be administered intramuscularly in the deltoid muscle of said patient; (2) a second reinitiation loading dose of the monthly injectable paliperidone palmitate depot to be administered in the deltoid muscle of said patient on about the 4th day to 20 about the 12th day after administering said first reinitiation loading dose; and (3) a reinitiation dose of the 3-month injectable paliperidone palmitate depot in the range of about 175mg eq. to about 525 mg eq. to be administered in the deltoid or gluteal muscle of said patient on about the 23rd day to about the 37th day after administering the second reinitiation loading dose of monthly injectable 25 paliperidone palmitate, wherein said first and second reinitiation loading dose and the reinitiation dose of the 3-month injectable paliperidone palmitate depot are selected from the table below based on the dose administered at the last injection of the 3-month injectable paliperidone palmitate depot Dose PP1M to be administered, two doses PP3M to be administered administered (into deltoid muscle) (into deltoid or gluteal muscle) at last injection of First Second Reinitiation Dose Reinitiation Dose Initiation Dose 175 mg eq. 50 mg eq. 50 mg eq. 175 mg eq. 263 mg eq. 75 mg eq. 75 mg eq. 263 mg eq. 350 mg eq. 100 mg eq. 100 mg eq. 350 mg eq. 525 mg eq. 100 mg eq. 100 mg eq. 525 mg eq. wherein the 1-month injectable paliperidone palmitate depot is a suspension of paliperidone palmitate having an average particle size of less than 2,000 nm to 100 nm; 5 wherein no intervening doses of paliperidone palmitate have been administered in between the last injection of the 3-month injectable paliperidone palmitate depot and the first reinitiation loading dose.
3. The use of an injectable paliperidone palmitate depot according to claim 1 or 2, wherein said patient is in need of treatment for psychosis.
4. The use of an injectable paliperidone palmitate depot according to claim 1 or 2, wherein said patient is in need of treatment for schizophrenia.
5. The use of an injectable paliperidone palmitate depot according to claim 1 or 2, wherein 15 said patient is in need of treatment for bipolar disorder.
6. The use of an injectable paliperidone palmitate depot according to claim 1 or 4, wherein the schizophrenia is a condition listed in DSM-IV-TR in category 295.xx. 20
7. The use of an injectable paliperidone palmitate depot according to claim 1 or 5, wherein the bipolar disorder is a condition listed in DSM-IV-TR in category 296.xx.
8. The use of an injectable paliperidone palmitate depot according to any one of claims 1-7, wherein said first reinitiation loading dose is to be administered on day 1 of treatment, said second reinitiation loading dose is to be administered on day 8 of treatment, and said reinitiation dose of the 3-month injectable paliperidone palmitate depot is to be administered one month after day 8 of treatment. 5
9. The use of an injectable paliperidone palmitate depot according to any one of claims 1-8, wherein the injectable paliperidone palmitate depot is formulated in an aqueous carrier.
10. A use of an injectable paliperidone palmitate depot according to any one of claims 10 1-9 substantially as herein described and with reference to any example thereof. PCT/US16/24841 252016 s vt? S i ! :x-'- KxMcs' 'jg* IF iiirs © "Cj £T5 ^ n F § ^c.::i ; <13 v*S> • KVV.'-V" xV-y ^jSXX.^ o o o o d d .,.-S fit ^-rs SUBSTITUTE SHEET (RULE 26) PCT/US16/24841 252016 ^ §*! $$$$ «l iw vNVsN £>;•; .^*«v m j&c ->{.»'• ® s? m ;> U>; sSiV ^1 %% i-S :Sw SS w '$§Q64 v^: ^ 4> I SWvi © ss- v " •' : r ess o O o o O o >vW W. Vv-.- • .s TT, >^- SUBSTITUTE SHEET (RULE 26) PCT/US16/24841 252016 <'»X' *13 sv$ « lso| CL 1 4- i Ci> ! i"** X ^ .•***••> !^s r« © t4^ -js J85 w» v' ;•«; j 12141 \vvs.' Cv ^""" Vx^sSi^ . sS«> w. o$ V«.v- t3 as i«J rs »«• $; , CN: ?vSjy^5f\j' o "o o o o o is <;::. || CB SUBSTITUTE SHEET (RULE 26) PCT/US16/24841 252016 Illustration 0f doamg; windows for RP1SVI m <52^ 5^^ a. £L £L '£L o> 0> E E ^v>> PPZ$ PPSM ppm C:< O a 0.. j » j s ^ : r months rnonlhs I^Jmspth- mont^- rnoritH Iniopth . | ^|VWVW<^' V*'->—j ^"VVWVSS^Wl-^lNS^ j ^.•VN^SNS^XSNVSN«IO ^VWNVX Ll_ZI I 4 days T dap ? days 7 ^ays 7: days 2 weeks 2 weeks SUBSTITUTE SHEET (RULE 26) IVHssecf dose for <4 rnoaths 15 'V^iks altar last dss^ J St H ->*yf********** Y*****"""'"' ©on^entratton * * i -o; X?j (ng/mU P •1! SZ).{ n| «^'< O 0,1- (5 5 £1317 41 §1 61 0 5 9131? 29 41 51 81 0 5 9131? 29 41 51 61 Time ('weeks} median paiipericlone concerdrations trDygli-peafe range before the I^RSM iJose was missad *ririr&im^rrrrrrrrrrrrr**^*****titititi*i*i^m'mirr&rrrrrrrr****f*r+t>t>r>t>t1i, vvii'rimfoivrrrrr&r*&r*********M'Mr**r*.'&rrrrrrrrrrrrrrr*r*rrr++**». wr***. i Months aflar last dose 4 Months .after last cfQsa ![ 6 Months aHar Mdssfe fvl^M ?fs •? Concsntfatson (ng/rnL} "^XsJ SS| I f ,, o! I . 1:.,., o3i,,. Q 1-1 wi 0 59 |i? 29 41 S1 61 71 81 1111:17 29 41 $'] S1 71 81 0 59 17 20 41 Sf ll 71 01 13 13 Time|weiks) —»msdiaii palipandQoe eoncentmtions H! pr64icio«-Merval$ gj Trough«Reak range bffqm the PP3fv1 dose was missed 1DO.O- Cdfieenirali^o *' * p (ng/rnL) Viw |S:j13) 29 I 51 | 71 j: P ] 111 |$p| a§ | SI f ft f il: I 111 !f p| 29 | 51 j T1 j 91 j ' 0 91? 41 SI .81 101 0. Ill 41 61 81 1Q1 0 917 41 61 81 101 Time (weeks) median pallperidone concentrations ^ Trpugli-peiksrange beforig the PP3y dose was misse#
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201562144054P | 2015-04-07 | 2015-04-07 | |
| US201562162596P | 2015-05-15 | 2015-05-15 | |
| NZ735952A NZ735952A (en) | 2015-04-07 | 2016-03-30 | Dosing regimen for missed doses for long-acting injectable paliperidone esters |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| NZ758246A NZ758246A (en) | 2024-05-31 |
| NZ758246B2 true NZ758246B2 (en) | 2024-09-03 |
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