RIMEGEPANT FOR CGRP RELATED DISORDERS
Disclosed are methods of treating CGRP related disorders, e.g., migraine, by administering to a patient in need thereof rimegepant or a pharmaceutically acceptable salt thereof. Pharmaceutical compositions comprising rimegepant and kits including the pharmaceutical compositions and instructions are also disclosed.
1 . A method of treating migraine in a patient in need thereof, comprising administering to the patient a pharmaceutical composition comprising a pharmaceutically acceptable carrier and a therapeutically effective amount of rimegepant, or a pharmaceutically acceptable salt thereof, in order to provide decrease in the number of migraines per month for said patient of at least 20%.
2 . The method of claim 1 wherein the decrease in the number of migraines per month for said patient of at least 30%.
3 . The method of claim 2 wherein the decrease in the number of migraines per month for said patient of at least 40%.
4 . A method of treating migraine in a patient in need thereof, comprising administering to the patient a pharmaceutical composition comprising a pharmaceutically acceptable carrier and a therapeutically effective amount of rimegepant, or a pharmaceutically acceptable salt thereof, in order to provide Pain Freedom of the pharmaceutical composition of at about 30% greater than placebo.
5 . The method of claim 1 wherein the Pain Freedom of the pharmaceutical composition is at least about 50% greater than placebo.
6 . The method of claim 4 wherein the Pain Freedom of the pharmaceutical composition is from about 30-75% greater than placebo.
7 . The method of claim 6 wherein the Pain Freedom of the pharmaceutical composition is from about 35-65% greater than placebo.
8 . A method of treating migraine in a patient in need thereof, comprising administering to the patient a pharmaceutical composition comprising a pharmaceutically acceptable carrier and a therapeutically effective amount of rimegepant, or a pharmaceutically acceptable salt thereof, in order to provide Freedom from MBS of the pharmaceutical composition of at about 30% greater than placebo.
9 . The method of claim 8 wherein the Freedom from MBS of the pharmaceutical composition is at least about 40% greater than placebo.
10 . The method of claim 8 wherein the Freedom from MBS of the pharmaceutical composition is from about 30-50% greater than placebo.
11 . The method of claim 4 which provides an AUCo —t of from about 80-125% of 5000 (hr*ng/mL).
12 . The method of claim 4 which provides a C max of from about 80-125% of 835 (ng/mL).
13 . A pharmaceutical composition comprising a pharmaceutically acceptable carrier and a therapeutically effective amount of rimegepant, or a pharmaceutically acceptable salt thereof, in order to provide an AUC 0-t of from about 80-125% of 5000 (hr*ng/mL).
14 . The pharmaceutical composition of claim 13 which comprises about 75 mg of rimegepant or a pharmaceutically acceptable salt thereof.
15 . The pharmaceutical composition of claim 13 wherein the rimegepant is in the form of a hemisulfate sesquihydrate salt.
16 . The pharmaceutical composition of claim 13 in the form of a tablet.
17 . The pharmaceutical composition of claim 16 comprising from about 50-60 wt % rimegepant hemisulfate sesquihydrate, about 30-35 wt % microcrystalline cellulose, about 2-7 wt % hydroxypropyl cellulose, about 3-7 wt % croscarmellose sodium, and about 0.1-1.0 wt % magnesium stearate.
18 . The pharmaceutical composition of claim 17 comprising about 57.1 wt % rimegepant hemisulfate sesquihydrate, about 33.4 wt % microcrystalline cellulose, about 4.0 wt % hydroxypropyl cellulose, about 5.0 wt % croscarmellose sodium, and about 0.5 wt % magnesium stearate.
19 . The pharmaceutical composition of claim 13 in the form of an oral solid molded fast-dispersing dosage form.
20 . The pharmaceutical composition of claim 19 comprising from about 70-80 wt % rimegepant hemisulfate sesquihydrate, about 10-20 wt % fish gelatin, about 10-20 wt % of a filler, and 0.1-5.0 wt % of a flavorant.
21 . The pharmaceutical composition of claim 20 wherein the filler is mannitol.