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1. WO2020118213 - METHODS FOR TREATING CANCER RESISTANT TO CDK4/6 INHIBITORS

Publication Number WO/2020/118213
Publication Date 11.06.2020
International Application No. PCT/US2019/065005
International Filing Date 06.12.2019
IPC
A61P 35/00 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35Antineoplastic agents
A61K 31/015 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
01Hydrocarbons
015carbocyclic
A61K 31/137 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
13Amines, e.g. amantadine
135having aromatic rings, e.g. methadone
137Arylalkylamines, e.g. amphetamine, epinephrine, salbutamol, ephedrine
A61K 31/138 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
13Amines, e.g. amantadine
135having aromatic rings, e.g. methadone
138Aryloxyalkylamines, e.g. propranolol, tamoxifen, phenoxybenzamine
A61K 45/06 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
45Medicinal preparations containing active ingredients not provided for in groups A61K31/-A61K41/132
06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
CPC
A61K 31/015
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
01Hydrocarbons
015carbocyclic
A61K 31/137
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
13Amines
135having aromatic rings ; , e.g. ketamine, nortriptyline
137Arylalkylamines, e.g. amphetamine, epinephrine, salbutamol, ephedrine ; or methadone
A61K 31/138
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
13Amines
135having aromatic rings ; , e.g. ketamine, nortriptyline
138Aryloxyalkylamines, e.g. propranolol, tamoxifen, phenoxybenzamine
A61K 45/06
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
45Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
A61P 35/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
35Antineoplastic agents
Applicants
  • RADIUS PHARMACEUTICALS, INC. [US]/[US]
Inventors
  • PATEL, Hitisha
  • BIHANI, Teeru
  • ARLT, Heike
  • TAO, Nianjun
Agents
  • DOYLE, Kathryn, D.
Priority Data
62/776,32306.12.2018US
Publication Language English (EN)
Filing Language English (EN)
Designated States
Title
(EN) METHODS FOR TREATING CANCER RESISTANT TO CDK4/6 INHIBITORS
(FR) MÉTHODES DE TRAITEMENT DU CANCER RÉSISTANT AUX INHIBITEURS CDK4/6
Abstract
(EN)
Disclosed herein are methods of treating a CDK4/6 inhibitor resistant estrogen receptor alpha-positive cancer in a subject having either a wild-type estrogen receptor alpha and/or a mutant estrogen receptor alpha, the method comprising administering to the subject a therapeutically effective amount of elacestrant, or a pharmaceutically acceptable salt or solvate thereof, wherein the mutant estrogen receptor alpha comprises one or more mutations selected from the group consisting of D538G, Y537X1, L536X2, P535H, V534E, S463P, V392I, E380Q and combinations thereof, wherein: X1 is S, N, or C; and X2 is R or Q. In some embodiments, the CDK4/6 inhibitor resistant estrogen receptor alpha-positive cancer is selected from the group consisting of breast cancer, uterine cancer, ovarian cancer, and pituitary cancer.
(FR)
L'invention concerne des méthodes de traitement d'un cancer positif au récepteur alpha des oestrogènes résistant à un inhibiteur de CDK4/6 chez un sujet ayant soit un récepteur alpha des oestrogènes de type sauvage et/ou un récepteur alpha des oestrogènes mutant, la méthode comprenant l'administration au sujet d'une quantité thérapeutiquement efficace d'élacestrant, ou d'un sel ou solvate pharmaceutiquement acceptable de celui-ci, le récepteur alpha des oestrogènes mutant comprenant une ou plusieurs mutations choisies dans le groupe constitué par D538G, Y537X1, L536X2, P535H, V534E, S463P, V392I, E380Q et des combinaisons de ceux-ci, où: X1 représente S, N ou C; et X2 représente R ou Q. Dans certains modes de réalisation, le cancer apositif au récepteur alpha des oestrogènes résistant aux inhibiteurs de CDK4/6 est choisi dans le groupe constitué par le cancer du sein, le cancer de l'utérus, le cancer de l'ovaire et le cancer de l'hypophyse.
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