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(12) Patent Application Publication (10) Pub. No.: US 2011/0105536A1 Lewyn-Briscoe Et Al

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(12) Patent Application Publication (10) Pub. No.: US 2011/0105536A1 Lewyn-Briscoe Et Al US 2011 01 05536A1 (19) United States (12) Patent Application Publication (10) Pub. No.: US 2011/0105536A1 Lewyn-Briscoe et al. (43) Pub. Date: May 5, 2011 (54) DOSING REGIMENASSOCATED WITH Publication Classification LONG-ACTING INUECTABLE PALIPERDONE ESTERS (51) Int. Cl. A 6LX 3/59 (2006.01) (76) Inventors: Peter H. Lewyn-Briscoe, A6IP 25/18 (2006.01) Newtown, PA (US); Cristiana Gassmann-Mayer, Pennington, NJ (US); Srihari Gopal, Belle Meade, (52) U.S. Cl. ................................................... S14/259.41 NJ (US); David W. Hough, Wallingford, PA (US); Bart M.M. Remmerie, Gent (BE); Mahesh N. (57) ABSTRACT Samtani, Flemington, NJ (US) The present application provides a method for treating (21) Appl. No.: 12/916,910 patients in need of psychiatric treatment, wherein said patient (22) Filed: Nov. 1, 2010 misses a stabilized dose of a monthly maintenance regimen of paliperidone palmitate. The present application also provides Related U.S. Application Data a method for treating psychiatric patients in need of a Switch (60) Provisional application No. 61/256,696, filed on Oct. ing treatment to paliperidone palmitate in a Sustained release 30, 2009. formulation. Patent Application Publication May 5, 2011 Sheet 1 of 6 US 2011/O105536 A1 FIG. 1 First-Order PrOCeSS Cp V CL Central (2) Zero-Order PrOCeSS Patent Application Publication May 5, 2011 Sheet 2 of 6 US 2011/O105536 A1 FIG. 2 25mgeq 50mgeq m-100mde::::: Missed doSe On WK 4. Patient returns On WK5 Missed doSe On WK 4. Patient returns On WK 6 -8-4 O 4 8 12 16 2024 -8-4 O 4 8 12 1620 24 Missed doSe On WK 4. Patient returns On WK7 Missed dose On WK4. Patient returns On WK 8 -8 -4 O 4 8 12 16 20 24 -8-4 O 4 8 12 16 20 24 Time (week) Patent Application Publication May 5, 2011 Sheet 4 of 6 US 2011/O105536 A1 (MM)?uu|| ?N?T?) Ø98373039|Z|870 1 (u/6u) uOleIllueOuOO Patent Application Publication May 5, 2011 Sheet 5 of 6 US 2011/O105536 A1 FIG. 5 Daily Extended Release Paliperidone (InVega 6mg) f 6-mg Invega Switched to 150/100mgeq. Pali-Palmitate Nikkijjilikikiikiikkilikikilikiddikikilik s - -7 1 8 15 22 29 Daily Extended Release Paliperidone (Invega 6mg) ITT 6-mg Invega Switched Over to 150mg eq, Pali-Palmitate u W iiikiikiikkidikkidikkidikkidikiki -7 1 8 15 22 29 Time (day) Patent Application Publication May 5, 2011 Sheet 6 of 6 US 2011/O105536 A1 FIG. 6 - 100 S d S 3 10 t E 9C 1 O O OCD O. > 4DOSes of 50mgeq. g Paliperidone Palmitate 5 < 0.01 4DOSes of 100 mg eq. Paliperidone Palmitate O 2 4 6 8 10 14 18 22 Time (wk) US 2011/O 105536 A1 May 5, 2011 DOSING REGIMENASSOCATED WITH 0007 Paliperidone palmitate is an atypical antipsychotic LONG-ACTING INUECTABLE drug administered by injection. Paliperidone palmitate may PALPERDONE ESTERS be administered at flexible injection sites including gluteal or deltoid muscle. Previous oil-based antipsychotic agents are CROSS REFERENCE TO RELATED indicated for gluteal muscle injection and may be associated APPLICATIONS with pain on injection, which may cause undesired effects of needle phobia and perceived injection pain. This may reduce 0001. This application claims the benefit of U.S. Provi patients’ acceptance towards these medications and resultina sional Application 61/256,696, filed on Oct. 30, 2009, which negative influence on the clinical management of these is incorporate by reference herein in its entirety. patients. The administration of paliperidone palmitate at flex ible injection sites may improve patients acceptance and FIELD OF THE INVENTION compliance to psychotic treatment. 0002 This invention relates to a method for treating 0008. In addition, paliperidone palmitate provides ben patients in need of Switching treatment from other antipsy efits of Sustained dose release in plasma without significant chotic drug to long-acting injectable paliperidone palmitate concentration variation, regular monitor, reduced side effects formulations. and increased treatment efficacy. The administration of pali peridone palmitate may improve effectiveness of psychotic BACKGROUND OF THE INVENTION treatment. 0003 Antipsychotic medications are the mainstay in the 0009. Therefore, there may be an increasing demand to treatment of Schizophrenia, Schizoaffective disorder, and switch treatment of patients in need thereof from oral or Schizophreniform disorders. Conventional antipsychotics injectable antipsychotic drugs to paliperidone palmitate. Fur were introduced in the mid-1950s. These typical or first gen ther, there is a need to reinitiate a dosing regimen for patients eration drugs are usually effective in controlling the positive who misses their maintenance or stabilized dose. Thus, the symptoms of Schizophrenia, but are less effective in moder objective of the present application is to provide a dosing ating the negative symptoms or the cognitive impairment regimen of paliperidone palmitate for patients in need of a associated with the disease. Atypical antipsychotics or sec treatment Switching from other antipsychotic agents to pali ond generation drugs, typified by risperidone and olanzapine, peridone palmitate. Another objective of the present applica were developed in the 1990s, and are generally characterized tion is to provide a dosing regimen of paliperidone palmitate by effectiveness against both the positive and negative symp for patients who have missed the monthly maintenance or toms associated with Schizophrenia. stabilized dosing regimen of paliperidone palmitate. 0004 Paliperidone palmitate is the palmitate ester of pali peridone (9-hydroxy-risperidone), a monoaminergic antago SUMMARY OF THE INVENTION nist that exhibits the characteristic dopamine D and seroto 0010. In one embodiment of the present application a dos nin (5-hydroxytryptamine type 2A) antagonism of the second ing regimen is provided for administering paliperidone generation, atypical antipsychotic drugs. Paliperidone is the palmitate to a patient in need of psychiatric treatment, major active metabolite of risperidone. Extended release wherein said patient misses a stabilized monthly maintenance (ER) osmotic controlled release oral delivery (OROS) pali dose for more than about 4 weeks and less than about 6 weeks, peridone, as a tablet formulation, is marketed in the United comprising administering intramuscularly in the deltoid a States (U.S.) for the treatment of schizophrenia and mainte first reinitiation loading dose of paliperidone as a paliperi nance of effect. done palmitate formulated in a Sustained release formulation 0005 Paliperidone palmitate is being developed as a long on the first day of treatment; and administering intramuscu acting, intramuscular (i.m.), injectable aqueous nanosuspen larly in the gluteal a reinitiation maintenance dose of paliperi sion for the treatment of schizophrenia and other related done as a paliperidone esterina Sustained release formulation diseases that are normally treated with antipsychotic medica on the 23 day to about the 37' day or between about 30+7 tions. Because of extreme low water solubility, paliperidone day after said first day of treatment. esters such as paliperidone palmitate dissolve slowly after an 0011. In another embodiment of the present application a i.m. injection before being hydrolyzed to paliperidone and dosing regimen is provided for administering paliperidone made available in the systemic circulation. esters to a patient in need of psychiatric treatment, wherein 0006. Many patients with the mental illnesses achieve said patient misses a stabilized monthly maintenance dose for symptom stability with available oral antipsychotic medica more than about 6 weeks, comprising administering intra tions; however, it is estimated that up to 75% have difficulty muscularly in the deltoid a first reinitiation loading dose of adhering to a daily oral treatment regimen, i.e. compliance paliperidone as a paliperidone palmitate formulated in a Sus problems. Problems with adherence often result in worsening tained release formulation on the first day of treatment; of symptoms, Suboptimal treatment response, frequent administering intramuscularly in the deltoid a second reini relapses and re-hospitalizations, and an inability to benefit tiation loading dose of paliperidone as a paliperidone palmi from rehabilitative and psychosocial therapies. Paliperidone tate formulated in a sustained release formulation 1 week palmitate injection has been developed to provide Sustained later (on the eighth day of treatment); and administering plasma concentrations of paliperidone when administered intramuscularly in the gluteal a reinitiation maintenance dose once monthly, which may greatly enhance compliance with of paliperidone as a paliperidone ester in a Sustained release dosing. Paliperidone palmitate formulated as an aqueous formulation on about the 23" day to about the 37' day or nanosuspension is described in U.S. Pat. Nos. 6,577.545 and between about 30+7 days after said first day of treatment. 6,555,544. In addition, a dosing regimen of paliperidone 0012. According to the present application, the first reini palmitate for treating patients is disclosed in US Patent Appli tiation dose and the second reinitiaiton dose may be the same cation Publication No. 20090163519. dosing as the stabilized monthly maintenance dose. Further, US 2011/O 105536 A1 May 5, 2011 the first reinitiation dose, the second reinitiation dose and the paliperidone palmitate on day 1 using the day 1/day8 initia reinitiation maintenance dose of paliperidone as a paliperi tion. (B) Hatched area represents patients switched to pali done
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