US20220249444A1 - Use of tradipitant in motion sickness - Google Patents

Use of tradipitant in motion sickness Download PDF

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US20220249444A1
US20220249444A1 US17/731,831 US202217731831A US2022249444A1 US 20220249444 A1 US20220249444 A1 US 20220249444A1 US 202217731831 A US202217731831 A US 202217731831A US 2022249444 A1 US2022249444 A1 US 2022249444A1
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Prior art keywords
tradipitant
motion sickness
effective amount
symptom
dose
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US17/731,831
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English (en)
Inventor
Mihael H. Polymeropoulos
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Vanda Pharmaceuticals Inc
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Vanda Pharmaceuticals Inc
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Priority claimed from US16/591,927 external-priority patent/US10821099B2/en
Application filed by Vanda Pharmaceuticals Inc filed Critical Vanda Pharmaceuticals Inc
Priority to US17/731,831 priority Critical patent/US20220249444A1/en
Assigned to VANDA PHARMACEUTICALS INC. reassignment VANDA PHARMACEUTICALS INC. ASSIGNMENT OF ASSIGNORS INTEREST (SEE DOCUMENT FOR DETAILS). Assignors: POLYMEROPOULOS, MIHAEL H.
Publication of US20220249444A1 publication Critical patent/US20220249444A1/en
Priority to US18/652,776 priority patent/US20240285588A1/en
Abandoned legal-status Critical Current

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    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4192—1,2,3-Triazoles
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/08—Drugs for disorders of the alimentary tract or the digestive system for nausea, cinetosis or vertigo; Antiemetics

Definitions

  • Tradipitant is a highly potent, selective, centrally penetrating, and orally active neurokinin-1 (NK-1) receptor antagonist, depicted below as the compound of Formula (I)
  • tradipitant produces a long-lasting blockade of brain NK-1 receptors. Although the distinct pathways of nausea and vomiting are largely undetermined, a definitive role of SP acting at NK-1 receptors in the nucleus tractus solitarus has been confirmed. Previous clinical studies have demonstrated the efficacy of NK-1 antagonism in the prevention of chemotherapy induced and post-operative nausea and vomiting (CINV and PONV).
  • a first aspect of the invention provides a method of prevention of motion sickness or one or more symptoms thereof, in an individual anticipating experiencing sickness-inducing motion, comprising administering tradipitant to said individual in an amount effective to prevent manifestation of motion sickness or one or more symptoms thereof.
  • the amount of tradipitant that is effective to prevent motion sickness or a symptom thereof may be, e.g., 100-400 mg, 100-300 mg, or 100-200 mg.
  • the effective amount can be about 170 mg.
  • the effective amount may be administered in a single dose, such as a single oral dose, and may or may not be in a single dosage unit form.
  • the dose may be administered in advance of engaging in a sickness-inducing motion, typically about 30 minutes before commencing such motion.
  • Administration of such an effective amount prior to commencing sickness-inducing motion can prevent or reduce the severity or frequency of one or more symptoms of motion sickness, including the prevention of nausea, vomiting, dizziness, headache, fullness, cold sweats, sweating, pallor, or disorientation.
  • a second aspect of the invention provides a method of treating motion sickness or one or more symptoms thereof, in an individual experiencing the manifestation of motion sickness, comprising administering tradipitant to said individual in an amount effective to treat the motion sickness or the symptom thereof.
  • Treatment of motion sickness may be considered to include a reduction in severity of symptoms, the prevention of progression, or the complete resolution of one or more symptoms of motion sickness after such symptom or symptoms have manifest in the individual.
  • the amount of tradipitant that is effective to treat motion sickness or a symptom thereof may be, e.g., 100-400 mg, 100-300 mg, or 100-200 mg.
  • the effective amount can be about 170 mg.
  • the effective amount may be administered in a single dose, such as a single oral dose, and may or may not be in a single dosage unit form.
  • the dose may be administered after the onset of at least one symptom of motion sickness, preferably soon after the onset of the at least one symptom, and more preferably, immediately after the onset of the at least one symptom.
  • Administration of such an effective amount after motion sickness has begun to manifest can reduce the severity of the symptom(s), eliminate the symptom(s), prevent the progression or intensification of the symptom(s) of motion sickness, for example from dizziness to nausea, from nausea to vomiting, etc.
  • a third aspect of the invention provides tradipitant for use in any of the methods of treatment or prevention described in the preceding aspects.
  • a fifth aspect of the invention provides tradipitant for use in the manufacture of a pharmaceutical composition comprising tradipitant for use in any of the preceding methods of treatment or prevention.
  • FIG. 2 illustrates the effect of tradipitant on NK-1 agonist (GR73632, 3 pmol, icv)-induced foot-tapping behavior after oral administration: comparison with other NK-1 antagonists, aprepitant and CP-122721: dose response.
  • FIG. 3 illustrates the effect of tradipitant on NK-1 agonist (GR73632, 3 pmol, icv)-induced foot-tapping behavior after oral administration: comparison with other NK-1 antagonists, aprepitant and CP-122721: time course.
  • FIG. 4 illustrates the effect of tradipitant on GR73632-induced vocalization in guinea pigs across a concentration range of 0.05 to 10 mg/kg.
  • the method of using tradipitant as described herein requires administering an amount of tradipitant that is effective to prevent or treat motion sickness or a symptom thereof.
  • the amount administered to a subject being treated depends upon a number of factors, including the species being treated, the weight of the subject being treated, and the subject's condition otherwise.
  • the method specifically involves the prevention and amelioration of motion sickness in human beings, including adult human beings. In adult human beings the typical dose effective to prevent motion sickness or a symptom thereof is 100-400 mg, 100-300 mg, or 100-200 mg.
  • One specific regime involves administration of about 85-170 mg, or more particularly about 170 mg.
  • the terms “patient,” “subject,” and “individual” refer to a mammal who is administrated tradipitant. Guinea pigs, dogs, cats, gerbils, horses, cattle, sheep, and humans are within the scope of the terms “patient,” “subject,” and “individual.” The most preferred subject is a human being.
  • the term “effective amount,” i.e., dose, of tradipitant refers to an amount that is effective in treating or preventing the disorders described herein, or symptoms thereof.
  • the amount of tradipitant that is effective to treat motion sickness or a symptom thereof may be, e.g., 100-400 mg, 100-300 mg, 100-200 mg, 85-170 mg, or particularly about 170 mg.
  • the effective amount may be administered in a single dose, including a single oral dose, which may or may not be in a single dosage unit form.
  • the effective amount of tradipitant may be administered after the onset of at least one symptom of motion sickness.
  • the effective amount is administered soon after the onset of the at least one symptom, for example up to thirty (30) minutes after the onset of the at least one symptom, and more preferably, the effective amount is administered immediately or substantially immediately after the onset of the at least one symptom.
  • Administration of such an effective amount after motion sickness has begun to manifest can reduce the severity of the symptom(s), eliminate the symptom(s), or prevent the progression or intensification of the symptom(s) of motion sickness, for example from dizziness to nausea, from nausea to vomiting, etc.
  • Tradipitant is a selective neurokinin-1 (NK-1) receptor antagonist.
  • NK-1 receptor antagonist a selective neurokinin-1 receptor antagonist.
  • tradipitant potently inhibits NK-1 receptor binding and antagonizes the effects of an NK-1 agonist in a functional assay. No significant activity is observed in a panel of 74 additional receptors, enzymes, and ion channels including the NK-2 and NK-3 receptors.
  • tradipitant is also a potent centrally active NK-1 antagonist in vivo.
  • results from tradipitant evaluation in a panel of 74 other receptors, enzymes, and ion channels indicate that, at a test concentration of 1 ⁇ M, tradipitant does not exhibit any inhibition of binding greater than 50%.
  • the compound produces no significant inhibition. Therefore, tradipitant is a highly selective NK-1 antagonist in vitro.
  • Example 1.2 Efficacy Models for In Vivo Evaluation of Brain NK-1 Receptor Occupancy and Efficacy of Tradipitant
  • NK-1 receptor antagonists Differences in species selectivity of NK-1 receptors pose challenges to characterization of NK-1 receptor antagonists in vivo.
  • Gerbil NK-1 receptors have previously been shown to be similar to those in humans. Gerbils exhibit a characteristic stereotypic foot-tapping behavior in response to distress, fear, or aversive stimuli.
  • Intracerebroventricular (icy) administration of substance P or a selective NK-1 receptor agonist such as GR73632 produces rapid rhythmic tapping of the hind feet lasting approximately 5 minutes, which can be inhibited by systemic administration of a brain penetrating antagonist of the NK-1 receptor.
  • This response is selective for NK-1 agonists, since selective NK-2 and NK-3 agonists do not elicit a similar response.
  • This behavioral response is further characterized and modified to enable identification and optimization, in vivo, of potent NK-1 receptor antagonists including tradipitant.
  • the San Diego Instruments “SR” DOS-based computer program is used on a PC to record the number of foot-taps over the following 6 to 10 minutes, beginning 30 seconds after the floor is lightly tapped.
  • Raw data are converted with a Microsoft® Excel® (Microsoft® and Excel® are registered trademarks of Microsoft Corp., Redmond, Wash.) macro that determines the number of events over threshold (125) in each 250-millisecond time bin over the 5.5 minutes following onset of observation. The total number and average intensity of events over the duration is determined. Total number of taps is analyzed with one-way ANOVA and post-hoc Dunnett's test using IMP statistical software.
  • a dose-response curve (with doses of 0.3, 1, 3 and 10 pmols, icy) is initially generated with the NK-1 agonist GR73632. Maximal foot-tapping behavior is achieved with 3 and 10 pmol doses; the 3 pmol dose is subsequently chosen as the dose of choice for antagonism experiments.
  • NK-1 antagonists are tested for their ability to attenuate GR73632-induced foot tapping. NK-1 antagonists are administered (po) via oral feeding tube at doses and time points specified in each experiment. All animals receive only one dose of NK-1 antagonists in all tests.
  • NK-1 antagonists are administered at multiple doses (at least 3; one dose per animal) and response to GR73632 is measured.
  • orally administered tradipitant potently inhibits NK-1 agonist-induced foot-tapping behavior in gerbils 2 hours after administration of drug in a dose-dependent manner, with an ED 50 of 0.03 ⁇ 0.004 mg/kg (*p ⁇ 0.05 compared to vehicle for 0.1 mg/kg and 0.3 mg/kg doses).
  • Data shown in FIG. 1 are expressed in number of foot-tapping events occurring in five (5) minutes.
  • FIG. 3 depicts the effects of tradipitant over a time course on NK-1 agonist (GR 73632, 3 pmol, icv)-induced foot-tapping behavior after oral administration, compared with that of NK-1 antagonists aprepitant and CP-122721.
  • Tradipitant 0.1 mg/kg, po
  • tradipitant shows greater than 50% inhibition of foot-tapping behavior 16 hours after administration.
  • the duration of effect of tradipitant is longer than that of CP-122721 (up to 2 hours after administration, 3 mg/kg) while aprepitant (1 mg/kg) shows inhibition of foot-tapping behavior up to 24 hours after administration. Data are expressed as percent control of vehicle (vehicle response to 3 pmol GR73632).
  • aprepitant a positive control
  • tradipitant a known emetic
  • Each animal is administered a different dose on a particular dosing day, so that each dose of tradipitant, aprepitant, and apomorphine alone is represented. Over the five (5) weeks of the study, each animal receives each of the treatments, but only one per week. The purpose of this study is to determine if tradipitant suppresses apomorphine-induced emesis.
  • the low dose of tradipitant is 10 times the ED 50 in the gerbil foot-tapping model of NK-1 receptor antagonism (Example 1.2.1).
  • the high dose is 100 times this efficacious dose, and is also the dose of aprepitant that has previously been determined to be efficacious against apomorphine-induced emesis in the dog.
  • the mid dose of tradipitant is the approximate half-log interval between the low and high doses.
  • the oral route of administration is selected for tradipitant because this is the route proposed or currently used clinically.
  • the intravenous route is typically used for experimental apomorphine administration.
  • the beagle dog is considered an effective species for demonstration of antagonism of apomorphine-induced emesis.
  • All dogs are fasted overnight prior to each treatment day and then fed approximately one (1) hour after oral dosing (approximately one (1) hour prior to administration of apomorphine). Individual doses are adjusted weekly for changes in body weight.
  • the dose regimen consists of a 5 ⁇ 5 Latin square design, in which each subject receives 1 dose or dose combination per week (6 day washout) as shown in Table 3 below.
  • Table 4 provides individual and mean and standard deviation values for the 2 hour plasma concentrations of tradipitant. All animals administered tradipitant have measurable levels at 2 hours post-dose. In general, plasma concentrations at 2 hours post-dose increase with increasing dose in a sub-proportional manner. As observed in other studies in dogs, the exposure to tradipitant is variable between animals. Individual animal data reveal no relationship between plasma concentrations and week of administration.
  • NK-1 receptor agonist substance P SP
  • This behavioral assay is used to demonstrate potency and CNS penetration of NK-1 antagonists in the guinea pig, a species that has receptor affinity for NK-1 antagonists that is similar to humans.
  • 0.1 mg/kg of tradipitant or vehicle solution is administered orally and then 2, 4, or 7 hours later, 0.1 nmol of GR73632 is administered into the cerebral ventricle as described above. Vocalizations are recorded and quantified as indicated above.
  • Vehicle solutions are either CMC ( FIG. 4 data) or an ethanol/emulphor solution ( FIGS. 5 and 6 ). Data is analyzed using one-tailed t-tests.
  • oral administration of tradipitant produces significant inhibition of agonist-induced vocalization at doses of 10 mg/kg (p ⁇ 0.001), 1.0 mg/kg (p ⁇ 0.001), 0.1 mg/kg (p ⁇ 0.001), and 0.05 mg/kg (p ⁇ 0.001).
  • Data shown parenthetically in FIG. 4 indicate percent of control response. Activity of tradipitant does not wane at the lower doses, indicating that even lower doses would be required to produce a dose response function.
  • a tracer NK-1 antagonist compound (GR205171) is used to evaluate the ability of other NK-1 antagonists to occupy the brain NK-1 receptors.
  • the test compounds are administered orally and the tracer compound is administered intravenously afterward.
  • the occupancy of the NK-1 receptors is evaluated by quantitating the amount of the tracer compound bound to the brain NK-1 receptors after increasing doses of the test compounds.
  • tradipitant has an estimated ED 50 of 0.04 mg/kg p.o. and is substantially more potent than the other antagonists evaluated.
  • a randomized, double blind, placebo-controlled clinical study of motion sickness is conducted, in which 126 human subjects (“study participants”), each having a prior history of motion sickness, are subjected to sea travel in the Pacific Ocean under varied weather conditions.
  • this invention can be seen to comprise one or more of the following illustrative embodiments:
  • a method of treating a subject about to engage in an activity involving sickness-inducing motion comprising: administering tradipitant to said subject, prior to the commencement of said activity, in an amount effective to prevent motion sickness or at least one symptom of motion sickness in said subject.
  • a method of treating a subject with motion sickness or at least one symptom of motion sickness comprising: administering tradipitant to said subject in an amount effective to treat said sickness or a symptom thereof.
  • the administration further comprises oral administration of the effective amount of tradipitant.
  • tradipitant administered to the subject is in a solid immediate release form such as a capsule or tablet comprising tradipitant and one or more pharmaceutically acceptable excipients.
  • Tradipitant for use in any of the preceding methods of treatment.
  • a pharmaceutical composition comprising tradipitant for use in any of the preceding methods.
  • Tradipitant for use in the manufacture of a pharmaceutical composition comprising tradipitant for use in any of the preceding methods.
  • the terms “first,” “second,” and the like do not denote any order, quantity, or importance, but rather are used to distinguish one element from another, and the terms “a” and “an” herein do not denote a limitation of quantity, but rather denote the presence of at least one of the referenced item.
  • the modifier “about” used in connection with a quantity is inclusive of the stated value and has the meaning dictated by the context (e.g., includes the degree of error associated with measurement of the particular quantity).
  • the suffix “(s)” as used herein is intended to include both the singular and the plural of the term that it modifies, thereby including one or more of that term (e.g., the metal(s) includes one or more metals).
  • Ranges disclosed herein are inclusive and independently combinable (e.g., ranges of “up to about 25 mg, or, more specifically, about 5 mg to about 20 mg,” is inclusive of the endpoints and all intermediate values of the ranges of “about 5 mg to about 25 mg,” etc.).

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US17/731,831 US20220249444A1 (en) 2018-09-28 2022-04-28 Use of tradipitant in motion sickness
US18/652,776 US20240285588A1 (en) 2018-09-28 2024-05-01 Use of tradipitant in motion sickness

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US201862737992P 2018-09-28 2018-09-28
US201962874927P 2019-07-16 2019-07-16
PCT/US2019/053107 WO2020069092A1 (en) 2018-09-28 2019-09-26 Use of tradipitant in motion sickness
US16/591,927 US10821099B2 (en) 2018-09-28 2019-10-03 Use of tradipitant in motion sickness
US17/034,419 US20210008037A1 (en) 2018-09-28 2020-09-28 Use of tradipitant in motion sickness
US17/731,831 US20220249444A1 (en) 2018-09-28 2022-04-28 Use of tradipitant in motion sickness

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ES2824552T3 (es) * 2015-03-04 2021-05-12 Vanda Pharmaceuticals Inc Método de tratamiento con tradipitant
JP7791832B2 (ja) 2020-03-26 2025-12-24 バンダ・ファーマシューティカルズ・インコーポレイテッド トラジピタントによる下気道感染症の治療
WO2023019084A1 (en) * 2021-08-12 2023-02-16 Vanda Pharmaceuticals Inc. Treatment of gastric accommodation with tradipitant
US20240350469A1 (en) 2021-08-31 2024-10-24 Vanda Pharmaceuticals Inc. Treatment of lower respiratory tract infection with tradipitant
AU2023413130A1 (en) 2022-12-21 2025-06-05 Vanda Pharmaceuticals Inc. Methods of treatment with tradipitant

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2005042515A1 (en) * 2003-10-24 2005-05-12 Eli Lilly And Company Novel crystalline forms of {2-[1-(3,5-bis-trifluoromethylbenzyl)-5-pyridin-4-yl-1h-[1,2,3]triazol-4-yl]-pyridin-3-yl}-(2-chlorophenyl)-methanone

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PT1035115E (pt) * 1999-02-24 2005-01-31 Hoffmann La Roche Derivados de 4-fenilpiridina e a sua utilizacao como antagonistas do receptor nk-1
AU2003230829B8 (en) * 2002-04-26 2008-12-11 Eli Lilly And Company Triazole derivatives as tachykinin receptor antagonists
EP2722045B1 (en) * 2009-11-18 2016-07-06 Helsinn Healthcare SA Compositions for treating centrally mediated nausea and vomiting
ES2824552T3 (es) * 2015-03-04 2021-05-12 Vanda Pharmaceuticals Inc Método de tratamiento con tradipitant
CN119074729A (zh) * 2017-11-17 2024-12-06 万达制药公司 使用川地匹坦治疗胃肠疾病的方法

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* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2005042515A1 (en) * 2003-10-24 2005-05-12 Eli Lilly And Company Novel crystalline forms of {2-[1-(3,5-bis-trifluoromethylbenzyl)-5-pyridin-4-yl-1h-[1,2,3]triazol-4-yl]-pyridin-3-yl}-(2-chlorophenyl)-methanone

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HRP20250097T1 (hr) 2025-03-28
CN111918701B (zh) 2024-08-02
BR112020015484A2 (pt) 2021-04-27
EP3856338A1 (en) 2021-08-04
NZ766397A (en) 2023-09-29
KR20250140634A (ko) 2025-09-25
ES3010832T3 (en) 2025-04-04
CA3089238A1 (en) 2020-04-02
EP4450126A3 (en) 2025-02-19
SI3856338T1 (sl) 2025-04-30
US20240285588A1 (en) 2024-08-29
IL281569A (en) 2021-05-31
HUE070000T2 (hu) 2025-04-28
AU2019348001A1 (en) 2020-08-06
AU2019348001B2 (en) 2023-09-21
EP4450126A2 (en) 2024-10-23
PT3856338T (pt) 2025-01-31
FI3856338T3 (fi) 2025-02-03
IL281569B2 (en) 2025-04-01
IL281569B1 (en) 2024-12-01
ZA202004594B (en) 2024-12-18
WO2020069092A1 (en) 2020-04-02
DK3856338T3 (da) 2025-02-10
CN111918701A (zh) 2020-11-10
MX2020008456A (es) 2020-09-25
KR20210067980A (ko) 2021-06-08
KR102863233B1 (ko) 2025-09-22

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