A phase 1, multicenter, open‐label study to evaluate the pharmacokinetics, safety, and tolerability of a single dose of rimegepant in children (aged ≥6 to <12 years) with a history of migraine.
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| Title: | A phase 1, multicenter, open‐label study to evaluate the pharmacokinetics, safety, and tolerability of a single dose of rimegepant in children (aged ≥6 to <12 years) with a history of migraine. |
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| Authors: | Lim, Chay Ngee (AUTHOR), Mo, Gary (AUTHOR), Bhardwaj, Rajinder (AUTHOR), Comisar, Craig M. (AUTHOR), Emerson, Beth L. (AUTHOR), Matschke, Kyle T. (AUTHOR), Fisniku, Ogert (AUTHOR), Bertz, Richard (AUTHOR), Croop, Robert (AUTHOR), Liu, Jing (AUTHOR) |
| Source: | Headache: The Journal of Head & Face Pain. Jan2026, Vol. 66 Issue 1, p202-212. 11p. |
| Subjects: | Patient safety, Research funding, Clinical trials, Oral drug administration, Descriptive statistics, Analgesics, Control groups, Pre-tests & post-tests, Pharmacokinetics, Research, Research methodology, Migraine, Drug tolerance, Regression analysis, Children |
| Abstract: | Objective: To evaluate pharmacokinetics (PK), safety, and tolerability of a weight‐adjusted dose of rimegepant orally disintegrating tablet (ODT) in children (aged ≥6 to <12 years) with a history of migraine. Background: Rimegepant 75 mg ODT is approved for acute treatment of migraine (with or without aura) and preventive treatment of episodic migraine in adults. Studies of rimegepant in pediatric populations have not been conducted to date. Methods: In this phase 1 open‐label study, a single dose of rimegepant ODT was administered, based on body weight, to children aged ≥6 to <12 years. Children with body weight ≥15 kg to ≤30 kg received 25 mg (group 1; n = 7), children >30 kg to ≤50 kg received 50 mg (2 × 25 mg; group 2; n = 9), and children >50 kg received 75 mg (group 3; n = 5). Blood samples were collected pre‐dose and 0.5, 1.25, 3.5, and 18 h post‐dose and then analyzed using a validated bioanalytical assay. Rimegepant PK parameters, including area under the plasma concentration–time curve (AUC) from time zero to infinity (AUCinf), AUC from time zero to 24 h after dosing, maximum plasma concentration (Cmax), and time to Cmax were estimated using a population PK approach in which pediatric PK data from this study were used to update a previous rimegepant population PK model developed with adult data. A safety follow‐up phone call was conducted 4 days after dosing. Results: Twenty participants with ≥1 post‐dose PK sample were included in PK analyses. All 21 participants treated were analyzed for safety. A majority of the study population was White (67%) and female (57%), had a median (range) age of 9.0 (6 to 11) years, and a mean (standard deviation) body weight of 37.7 (12.3) kg. Geometric mean estimates of Cmax and AUCinf ranged from 615.9 to 811.1 ng/mL and 1987.8 to 4244.9 ng*h/mL, respectively, across weight groups. Rimegepant exposures, particularly AUCinf values, were lower in the two lower‐weight groups (groups 1 and 2) than in the higher‐weight group (group 3). Median time to Cmax was 1 to 1.5 h across weight/dose groups. Three (14%) participants (all in group 3) had ≥1 adverse event; all were mild in severity. No clinically relevant findings regarding laboratory tests, vital signs, electrocardiograms, physical examinations, local tolerability assessments, or the Sheehan‐Suicidality Tracking Scale were observed. Conclusions: A single weight‐adjusted dose of rimegepant ODT demonstrated a favorable safety profile in children aged ≥6 to <12 years with a history of migraine. Exposures in children >50 kg receiving 75 mg rimegepant were similar to observed exposures in adults receiving 75 mg. However, exposures in children >30 kg to ≤50 kg receiving 50 mg rimegepant and in children ≥15 kg to ≤30 kg receiving 25 mg rimegepant were lower than exposures in adults receiving 75 mg. These findings will be the basis for further refinement of pediatric dose in future studies. Plain Language Summary: This study looked at how rimegepant acts in the blood following a single weight‐adjusted dose among children aged aged 6 to less than 12 years to learn about the optimum dose for children. The amount of rimegepant in the blood was similar in children weighing more than 50 kg given a 75 mg dose compared to adults given the recommended dose of 75 mg; however, the amount of rimegepant in the blood was lower in children weighing between 30 and 50 kg given 50 mg of rimegepant and in children weighing between 15 and 30 kg given 25 mg of rimegepant. These findings demonstrate that further refinement of rimegepant dosing in children is required. [ABSTRACT FROM AUTHOR] |
| Copyright of Headache: The Journal of Head & Face Pain is the property of Wiley-Blackwell and its content may not be copied or emailed to multiple sites without the copyright holder's express written permission. Additionally, content may not be used with any artificial intelligence tools or machine learning technologies. However, users may print, download, or email articles for individual use. This abstract may be abridged. No warranty is given about the accuracy of the copy. Users should refer to the original published version of the material for the full abstract. (Copyright applies to all Abstracts.) | |
| Database: | Psychology and Behavioral Sciences Collection |
| FullText | Text: Availability: 0 |
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| Header | DbId: pbh DbLabel: Psychology and Behavioral Sciences Collection An: 191181520 AccessLevel: 6 PubType: Academic Journal PubTypeId: academicJournal PreciseRelevancyScore: 0 |
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| Items | – Name: Title Label: Title Group: Ti Data: A phase 1, multicenter, open‐label study to evaluate the pharmacokinetics, safety, and tolerability of a single dose of rimegepant in children (aged ≥6 to <12 years) with a history of migraine. – Name: Author Label: Authors Group: Au Data: <searchLink fieldCode="AR" term="%22Lim%2C+Chay+Ngee%22">Lim, Chay Ngee</searchLink> (AUTHOR)<br /><searchLink fieldCode="AR" term="%22Mo%2C+Gary%22">Mo, Gary</searchLink> (AUTHOR)<br /><searchLink fieldCode="AR" term="%22Bhardwaj%2C+Rajinder%22">Bhardwaj, Rajinder</searchLink> (AUTHOR)<br /><searchLink fieldCode="AR" term="%22Comisar%2C+Craig+M%2E%22">Comisar, Craig M.</searchLink> (AUTHOR)<br /><searchLink fieldCode="AR" term="%22Emerson%2C+Beth+L%2E%22">Emerson, Beth L.</searchLink> (AUTHOR)<br /><searchLink fieldCode="AR" term="%22Matschke%2C+Kyle+T%2E%22">Matschke, Kyle T.</searchLink> (AUTHOR)<br /><searchLink fieldCode="AR" term="%22Fisniku%2C+Ogert%22">Fisniku, Ogert</searchLink> (AUTHOR)<br /><searchLink fieldCode="AR" term="%22Bertz%2C+Richard%22">Bertz, Richard</searchLink> (AUTHOR)<br /><searchLink fieldCode="AR" term="%22Croop%2C+Robert%22">Croop, Robert</searchLink> (AUTHOR)<br /><searchLink fieldCode="AR" term="%22Liu%2C+Jing%22">Liu, Jing</searchLink> (AUTHOR) – Name: TitleSource Label: Source Group: Src Data: <searchLink fieldCode="JN" term="%22Headache%3A+The+Journal+of+Head+%26+Face+Pain%22">Headache: The Journal of Head & Face Pain</searchLink>. Jan2026, Vol. 66 Issue 1, p202-212. 11p. – Name: Subject Label: Subjects Group: Su Data: <searchLink fieldCode="DE" term="%22Patient+safety%22">Patient safety</searchLink><br /><searchLink fieldCode="DE" term="%22Research+funding%22">Research funding</searchLink><br /><searchLink fieldCode="DE" term="%22Clinical+trials%22">Clinical trials</searchLink><br /><searchLink fieldCode="DE" term="%22Oral+drug+administration%22">Oral drug administration</searchLink><br /><searchLink fieldCode="DE" term="%22Descriptive+statistics%22">Descriptive statistics</searchLink><br /><searchLink fieldCode="DE" term="%22Analgesics%22">Analgesics</searchLink><br /><searchLink fieldCode="DE" term="%22Control+groups%22">Control groups</searchLink><br /><searchLink fieldCode="DE" term="%22Pre-tests+%26+post-tests%22">Pre-tests & post-tests</searchLink><br /><searchLink fieldCode="DE" term="%22Pharmacokinetics%22">Pharmacokinetics</searchLink><br /><searchLink fieldCode="DE" term="%22Research%22">Research</searchLink><br /><searchLink fieldCode="DE" term="%22Research+methodology%22">Research methodology</searchLink><br /><searchLink fieldCode="DE" term="%22Migraine%22">Migraine</searchLink><br /><searchLink fieldCode="DE" term="%22Drug+tolerance%22">Drug tolerance</searchLink><br /><searchLink fieldCode="DE" term="%22Regression+analysis%22">Regression analysis</searchLink><br /><searchLink fieldCode="DE" term="%22Children%22">Children</searchLink> – Name: Abstract Label: Abstract Group: Ab Data: Objective: To evaluate pharmacokinetics (PK), safety, and tolerability of a weight‐adjusted dose of rimegepant orally disintegrating tablet (ODT) in children (aged ≥6 to <12 years) with a history of migraine. Background: Rimegepant 75 mg ODT is approved for acute treatment of migraine (with or without aura) and preventive treatment of episodic migraine in adults. Studies of rimegepant in pediatric populations have not been conducted to date. Methods: In this phase 1 open‐label study, a single dose of rimegepant ODT was administered, based on body weight, to children aged ≥6 to <12 years. Children with body weight ≥15 kg to ≤30 kg received 25 mg (group 1; n = 7), children >30 kg to ≤50 kg received 50 mg (2 × 25 mg; group 2; n = 9), and children >50 kg received 75 mg (group 3; n = 5). Blood samples were collected pre‐dose and 0.5, 1.25, 3.5, and 18 h post‐dose and then analyzed using a validated bioanalytical assay. Rimegepant PK parameters, including area under the plasma concentration–time curve (AUC) from time zero to infinity (AUCinf), AUC from time zero to 24 h after dosing, maximum plasma concentration (Cmax), and time to Cmax were estimated using a population PK approach in which pediatric PK data from this study were used to update a previous rimegepant population PK model developed with adult data. A safety follow‐up phone call was conducted 4 days after dosing. Results: Twenty participants with ≥1 post‐dose PK sample were included in PK analyses. All 21 participants treated were analyzed for safety. A majority of the study population was White (67%) and female (57%), had a median (range) age of 9.0 (6 to 11) years, and a mean (standard deviation) body weight of 37.7 (12.3) kg. Geometric mean estimates of Cmax and AUCinf ranged from 615.9 to 811.1 ng/mL and 1987.8 to 4244.9 ng*h/mL, respectively, across weight groups. Rimegepant exposures, particularly AUCinf values, were lower in the two lower‐weight groups (groups 1 and 2) than in the higher‐weight group (group 3). Median time to Cmax was 1 to 1.5 h across weight/dose groups. Three (14%) participants (all in group 3) had ≥1 adverse event; all were mild in severity. No clinically relevant findings regarding laboratory tests, vital signs, electrocardiograms, physical examinations, local tolerability assessments, or the Sheehan‐Suicidality Tracking Scale were observed. Conclusions: A single weight‐adjusted dose of rimegepant ODT demonstrated a favorable safety profile in children aged ≥6 to <12 years with a history of migraine. Exposures in children >50 kg receiving 75 mg rimegepant were similar to observed exposures in adults receiving 75 mg. However, exposures in children >30 kg to ≤50 kg receiving 50 mg rimegepant and in children ≥15 kg to ≤30 kg receiving 25 mg rimegepant were lower than exposures in adults receiving 75 mg. These findings will be the basis for further refinement of pediatric dose in future studies. Plain Language Summary: This study looked at how rimegepant acts in the blood following a single weight‐adjusted dose among children aged aged 6 to less than 12 years to learn about the optimum dose for children. The amount of rimegepant in the blood was similar in children weighing more than 50 kg given a 75 mg dose compared to adults given the recommended dose of 75 mg; however, the amount of rimegepant in the blood was lower in children weighing between 30 and 50 kg given 50 mg of rimegepant and in children weighing between 15 and 30 kg given 25 mg of rimegepant. These findings demonstrate that further refinement of rimegepant dosing in children is required. [ABSTRACT FROM AUTHOR] – Name: AbstractSuppliedCopyright Label: Group: Ab Data: <i>Copyright of Headache: The Journal of Head & Face Pain is the property of Wiley-Blackwell and its content may not be copied or emailed to multiple sites without the copyright holder's express written permission. Additionally, content may not be used with any artificial intelligence tools or machine learning technologies. However, users may print, download, or email articles for individual use. This abstract may be abridged. No warranty is given about the accuracy of the copy. Users should refer to the original published version of the material for the full abstract.</i> (Copyright applies to all Abstracts.) |
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| RecordInfo | BibRecord: BibEntity: Identifiers: – Type: doi Value: 10.1111/head.15074 Languages: – Code: eng Text: English PhysicalDescription: Pagination: PageCount: 11 StartPage: 202 Subjects: – SubjectFull: Patient safety Type: general – SubjectFull: Research funding Type: general – SubjectFull: Clinical trials Type: general – SubjectFull: Oral drug administration Type: general – SubjectFull: Descriptive statistics Type: general – SubjectFull: Analgesics Type: general – SubjectFull: Control groups Type: general – SubjectFull: Pre-tests & post-tests Type: general – SubjectFull: Pharmacokinetics Type: general – SubjectFull: Research Type: general – SubjectFull: Research methodology Type: general – SubjectFull: Migraine Type: general – SubjectFull: Drug tolerance Type: general – SubjectFull: Regression analysis Type: general – SubjectFull: Children Type: general Titles: – TitleFull: A phase 1, multicenter, open‐label study to evaluate the pharmacokinetics, safety, and tolerability of a single dose of rimegepant in children (aged ≥6 to <12 years) with a history of migraine. Type: main BibRelationships: HasContributorRelationships: – PersonEntity: Name: NameFull: Lim, Chay Ngee – PersonEntity: Name: NameFull: Mo, Gary – PersonEntity: Name: NameFull: Bhardwaj, Rajinder – PersonEntity: Name: NameFull: Comisar, Craig M. – PersonEntity: Name: NameFull: Emerson, Beth L. – PersonEntity: Name: NameFull: Matschke, Kyle T. – PersonEntity: Name: NameFull: Fisniku, Ogert – PersonEntity: Name: NameFull: Bertz, Richard – PersonEntity: Name: NameFull: Croop, Robert – PersonEntity: Name: NameFull: Liu, Jing IsPartOfRelationships: – BibEntity: Dates: – D: 01 M: 01 Text: Jan2026 Type: published Y: 2026 Identifiers: – Type: issn-print Value: 00178748 Numbering: – Type: volume Value: 66 – Type: issue Value: 1 Titles: – TitleFull: Headache: The Journal of Head & Face Pain Type: main |
| ResultId | 1 |
