[go: up one dir, main page]

WO2025203012A1 - Inhibiteur de kras g12c destiné à être utilisé dans le traitement du cancer du poumon non à petites cellules - Google Patents

Inhibiteur de kras g12c destiné à être utilisé dans le traitement du cancer du poumon non à petites cellules

Info

Publication number
WO2025203012A1
WO2025203012A1 PCT/IB2025/090001 IB2025090001W WO2025203012A1 WO 2025203012 A1 WO2025203012 A1 WO 2025203012A1 IB 2025090001 W IB2025090001 W IB 2025090001W WO 2025203012 A1 WO2025203012 A1 WO 2025203012A1
Authority
WO
WIPO (PCT)
Prior art keywords
treatment
compound
methyl
nsclc
pembrolizumab
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Pending
Application number
PCT/IB2025/090001
Other languages
English (en)
Inventor
Rafael Caparica BITTON
Xiaoming Cui
Chiara LOBETTI BODONI
Alejandro Javier YOVINE
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Novartis AG
Original Assignee
Novartis AG
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Novartis AG filed Critical Novartis AG
Publication of WO2025203012A1 publication Critical patent/WO2025203012A1/fr
Pending legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • 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
    • A61K31/415—1,2-Diazoles
    • A61K31/416—1,2-Diazoles condensed with carbocyclic ring systems, e.g. indazole
    • 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • 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
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K33/00—Medicinal preparations containing inorganic active ingredients
    • A61K33/24—Heavy metals; Compounds thereof
    • A61K33/243—Platinum; Compounds thereof
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K39/00—Medicinal preparations containing antigens or antibodies
    • A61K39/395—Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K16/00—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies
    • C07K16/18—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans
    • C07K16/28—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
    • C07K16/2803—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants against the immunoglobulin superfamily
    • C07K16/2818—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants against the immunoglobulin superfamily against CD28 or CD152
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K39/00—Medicinal preparations containing antigens or antibodies
    • A61K2039/545—Medicinal preparations containing antigens or antibodies characterised by the dose, timing or administration schedule

Definitions

  • the present invention relates to a method of treating non-small cell lung cancer (NSCLC) which harbors a KRAS G12C mutation, wherein the method comprises the administration of a therapeutically effective amount of KRAS G12C inhibitor 1- ⁇ 6-[(4M)-4-(5-Chloro-6-methyl- 1 H-indazol-4-yl)-5-methyl-3-(1 -methyl-1 H-indazol-5-yl)-1 H-pyrazol-1 -yl]-2- azaspiro[3.3]heptan-2-yl ⁇ prop-2-en-1-one (Compound A), or a pharmaceutically acceptable salt, solvate or hydrate thereof, a therapeutically effective amount of pembrolizumab, a therapeutically effective amount of pemetrexed and a therapeutically effective amount of platinum therapy; in particular the present invention relates to a method of treating NSCLC wherein the NSCLC expresses at least 1% PD-L1 according to the tumor proportion score (TPS), more particularly where
  • RTKs Receptor Tyrosine Kinases
  • KRAS at codon 12 impair GTPase-activating protein (GAP)-stimulated GTP hydrolysis.
  • GAP GTPase-activating protein
  • Non-small cell lung cancer accounts for about 85% of all lung cancer diagnoses.
  • KRAS mutations are detected in approximately 25% of patients with lung adenocarcinomas (Sequist et al., 201 1 , Ann. Oncol., 22(12): 2616-24). They are most commonly seen at codon 12, with KRAS G12C mutations being most common (40% overall) in both adenocarcinoma and NSCLC.
  • the presence of KRAS mutations is prognostic of poor survival and has been associated with reduced responsiveness to EGFR TKI treatment.
  • a method of treating non-small cell lung cancer (NSCLC) in a subject in need thereof, and which cancer harbors a KRAS G12C mutation comprises administering to the subject a therapeutically effective amount of 1 - ⁇ 6-[(4M)-4-(5-Chloro-6-methyl-1 H- indazol-4-yl)-5-methyl-3-(1 -methyl-1 H-indazol-5-yl)-1 H-pyrazol-1 -yl]-2-azaspiro[3.3]heptan-2- yl ⁇ prop-2-en-1-one (Compound A), or a pharmaceutically acceptable salt, solvate or hydrate thereof, a therapeutically effective amount of pembrolizumab, a therapeutically effective amount of pemetrexed and a therapeutically effective amount of platinum therapy.
  • NSCLC non-small cell lung cancer
  • the invention provides a compound 1- ⁇ 6-[(4M)-4-(5-Chloro-6-methyl- 1 H-indazol-4-yl)-5-methyl-3-(1 -methyl-1 H-indazol-5-yl)-1 H-pyrazol-1 -yl]-2- azaspiro[3.3]heptan-2-yl ⁇ prop-2-en-1-one (Compound A), or a pharmaceutically acceptable salt, solvate or hydrate thereof, for use in a method of treating NSCLC wherein the method comprises administering to the subject a therapeutically effective amount of 1- ⁇ 6-[(4M)-4-(5- Chloro-6-methyl-1 H-indazol-4-yl)-5-methyl-3-(1 -methyl-1 H-indazol-5-yl)-1 H-pyrazol-1 -yl]-2- azaspiro[3.3]heptan-2-yl ⁇ prop-2-en-1-one (Compound A), or a pharmaceutically acceptable salt,
  • the invention provides the use of compound 1- ⁇ 6-[(4M)-4-(5-Chloro- 6-methyl-1 H-indazol-4-yl)-5-methyl-3-(1 -methyl-1 H-indazol-5-yl)-1 H-pyrazol-1 -yl]-2- azaspiro[3.3]heptan-2-yl ⁇ prop-2-en-1-one (Compound A), or a pharmaceutically acceptable salt, solvate or hydrate thereof, in the manufacture of a medicine for a method of treating NSCLC wherein the method comprises administering to the subject a therapeutically effective amount of 1- ⁇ 6-[(4M)-4-(5-Chloro-6-methyl-1 H-indazol-4-yl)-5-methyl-3-(1-methyl- 1 H-indazol-5-yl)-1 H-pyrazol-1 -yl]-2-azaspiro[3.3]heptan-2-yl ⁇ prop-2-en-1 -one (Compound A), or a
  • the invention provides a pharmaceutical combination comprising 1 - ⁇ 6-[(4M)-4-(5-Chloro-6-methyl-1 H-indazol-4-yl)-5-methyl-3-(1 -methyl-1 H-indazol-5-yl)-1 H- pyrazol-1-yl]-2-azaspiro[3.3]heptan-2-yl ⁇ prop-2-en-1-one (Compound A), or a pharmaceutically acceptable salt, solvate or hydrate thereof, a therapeutically effective amount of pembrolizumab, a therapeutically effective amount of pemetrexed and a therapeutically effective amount of platinum therapy.
  • CT computerized tomography; PET, positron emission tomography. Arrows indicate sites of tumor.
  • KRAS G12C inhibitor Compound A (INN: opnurasib):
  • Compound A is KRAS G12C inhibitor with the chemical name 1- ⁇ 6-[(4M)-4-(5-Chloro-6- methyl-1 H-indazol-4-yl)-5-methyl-3-(1 -methyl-1 H-indazol-5-yl)- 1 H-pyrazol-1 -yl]-2- azaspiro[3.3]heptan-2-yl ⁇ prop-2-en-1-one.
  • Compound A is also known by the chemical name a(R)-1 -(6-(4-(5-chloro-6-methyl-1 H-indazol-4-yl)-5-methyl-3-(1 -methyl-1 H-indazol-5-yl)-1 H- pyrazol-1-yl)-2-azaspiro[3.3]heptan-2-yl)prop-2-en-1-one.
  • Compound A is an atropisomer.
  • “Overall survival” is defined as the number of days between the date of start of study treatment to the date of death due to any cause. If no death is reported prior to study termination or analysis cut off, survival will be censored at the date of last known date patient alive prior to/on the cut-off date. Survival time for patients with no post-baseline survival information will be censored at the date of start of treatment.
  • PD Progressive Disease
  • SD Stable Disease
  • Compound A is also intended to represent unlabeled forms as well as isotopically labeled forms of the compounds.
  • Isotopically labeled compounds have one or more atoms replaced by an atom having a selected atomic mass or mass number.
  • isotopes that can be incorporated include isotopes, where possible, of hydrogen, carbon, nitrogen, oxygen, and chlorine, for example, 2H, 3H, 11C, 13C, 14C, 15N, 35S, 36CI.
  • Isotopically labelled compounds are useful in metabolic studies (with 14C), reaction kinetic studies (with, for example 2H or 3H), detection or imaging techniques, such as positron emission tomography (PET) or single-photon emission computed tomography (SPECT) including drug or substrate tissue distribution assays, or in radioactive treatment of patients.
  • Isotopically-labeled Compound A can generally be prepared by conventional techniques known to those skilled in the art using appropriate isotopically-labeled reagents.
  • isotopic enrichment factor means the ratio between the isotopic abundance and the natural abundance of a specified isotope.
  • a methyl group e.g. on the indazolyl ring, may be deuterated or perdeuterated.
  • Deuterated compounds of Compound A are described in CN116478141 B.
  • the present invention provides pharmaceutically acceptable compositions which comprise a therapeutically effective amount of Compound A, formulated together with one or more pharmaceutically acceptable carriers (additives) and/or diluents.
  • pharmaceutically acceptable carriers are sterile.
  • the pharmaceutical composition can be formulated for particular routes of administration such as oral administration, parenteral administration, and rectal administration, etc.
  • the pharmaceutical compositions of the present invention can be made up in a solid form (including without limitation capsules, tablets, pills, granules, powders or suppositories), or in a liquid form (including without limitation solutions, suspensions or emulsions).
  • the pharmaceutical compositions can be subjected to conventional pharmaceutical operations such as sterilization and/or can contain conventional inert diluents, lubricating agents, or buffering agents, as well as adjuvants, such as preservatives, stabilizers, wetting agents, emulsifiers and buffers, etc.
  • the pharmaceutical compositions are tablets or gelatin capsules comprising the active ingredient together with one or more of: a) diluents, e.g., lactose, dextrose, sucrose, mannitol, sorbitol, cellulose and/or glycine; b) lubricants, e.g., silica, talcum, stearic acid, its magnesium or calcium salt and/or polyethyleneglycol; c) binders, e.g., magnesium aluminum silicate, starch paste, gelatin, tragacanth, methylcellulose, sodium carboxymethylcellulose and/or polyvinylpyrrolidone; d) disintegrants, e.g., starches, agar, alginic acid or its sodium salt, or effervescent mixtures; and e) absorbents, colorants, flavors and sweeteners.
  • diluents e.g., lactose, dextrose, sucrose, mann
  • the pharmaceutical compositions are capsules comprising the active ingredient only.
  • Tablets may be either film coated or enteric coated according to methods known in the art.
  • compositions for oral administration include an effective amount of a compound in a combination of the invention in the form of tablets, lozenges, aqueous or oily suspensions, dispersible powders or granules, emulsion, hard or soft capsules, or syrups or elixirs, solutions or solid dispersion.
  • Compositions intended for oral use are prepared according to any method known in the art for the manufacture of pharmaceutical compositions and such compositions can contain one or more agents selected from the group consisting of sweetening agents, flavoring agents, coloring agents and preserving agents in order to provide pharmaceutically elegant and palatable preparations. Tablets may contain the active ingredient in admixture with nontoxic pharmaceutically acceptable excipients which are suitable for the manufacture of tablets.
  • excipients are, for example, inert diluents, such as calcium carbonate, sodium carbonate, lactose, calcium phosphate or sodium phosphate; granulating and disintegrating agents, for example, corn starch, or alginic acid; binding agents, for example, starch, gelatin or acacia; and lubricating agents, for example magnesium stearate, stearic acid or talc.
  • the tablets are uncoated or coated by known techniques to delay disintegration and absorption in the gastrointestinal tract and thereby provide a sustained action over a longer period.
  • a time delay material such as glyceryl monostearate or glyceryl distearate can be employed.
  • Formulations for oral use can be presented as hard gelatin capsules wherein the active ingredient is mixed with an inert solid diluent, for example, calcium carbonate, calcium phosphate or kaolin, or as soft gelatin capsules wherein the active ingredient is mixed with water or an oil medium, for example, peanut oil, liquid paraffin or olive oil.
  • an inert solid diluent for example, calcium carbonate, calcium phosphate or kaolin
  • water or an oil medium for example, peanut oil, liquid paraffin or olive oil.
  • compositions are aqueous isotonic solutions or suspensions, and suppositories are advantageously prepared from fatty emulsions or suspensions.
  • Said compositions may be sterilized and/or contain adjuvants, such as preserving, stabilizing, wetting or emulsifying agents, solution promoters, salts for regulating the osmotic pressure and/or buffers. In addition, they may also contain other therapeutically valuable substances.
  • Said compositions are prepared according to conventional mixing, granulating or coating methods, respectively, and contain about 0.1-75%, or contain about 1-50%, of the active ingredient.
  • compositions for transdermal application include an effective amount of a compound of the invention with a suitable carrier.
  • Carriers suitable fortransdermal delivery include absorbable pharmacologically acceptable solvents to assist passage through the skin of the host.
  • transdermal devices are in the form of a bandage comprising a backing member, a reservoir containing the compound optionally with carriers, optionally a rate controlling barrier to deliver the compound of the skin of the host at a controlled and predetermined rate over a prolonged period of time, and means to secure the device to the skin.
  • compositions for topical application include aqueous solutions, suspensions, ointments, creams, gels or sprayable formulations, e.g., for delivery by aerosol or the like.
  • topical delivery systems will in particular be appropriate for dermal application, e.g., for the treatment of skin cancer, e.g., for prophylactic use in sun creams, lotions, sprays and the like. They are thus particularly suited for use in topical, including cosmetic, formulations well-known in the art.
  • Such may contain solubilizers, stabilizers, tonicity enhancing agents, buffers and preservatives.
  • a topical application may also pertain to an inhalation or to an intranasal application. They may be conveniently delivered in the form of a dry powder (either alone, as a mixture, for example a dry blend with lactose, or a mixed component particle, for example with phospholipids) from a dry powder inhaler or an aerosol spray presentation from a pressurized container, pump, spray, atomizer or nebulizer, with or without the use of a suitable propellant.
  • a dry powder either alone, as a mixture, for example a dry blend with lactose, or a mixed component particle, for example with phospholipids
  • Products provided as a combined preparation include a composition comprising the compound of the present invention in the form of a kit.
  • the kit comprises means for separately retaining said compositions, such as a container, divided bottle, or divided foil packet.
  • a container such as a container, divided bottle, or divided foil packet.
  • An example of such a kit is a blister pack, as typically used for the packaging of tablets, capsules and the like.
  • the kit of the invention typically comprises directions for administration.
  • Pembrolizumab has been approved by the Food and Drug Administration (FDA) for treating NSCLC for the following indications:
  • TPS tumor proportion score
  • the recommended dose for pembrolizumab for treating NSCLC is 200 mg administered as an intravenous infusion over 30 minutes every 3 weeks until disease progression until disease progression, unacceptable toxicity, or up to 24 months in patients without disease progression.
  • Cisplatin is FDA approved for the treatment of advanced ovarian cancer, testicular cancer, and bladder carcinoma. However, clinicians frequently use cisplatin off-label for a number of other malignancies, as detailed below, when the benefits may outweigh the risks of adverse drug effects.
  • Example 1 Clinical efficacy of Compound A
  • the recommended dose for the monotherapy is a dose of 200 mg of Compound A taken orally twice daily (BID).
  • NE not evaluable
  • NSCLC non-small cell lung cancer
  • ORR overall response rate
  • PD progressive disease
  • PR partial response
  • QD once daily.
  • Figure 1 shows PET scans showing a substantial reduction in the 2-[fluorine-18]-fluoro-2- deoxy-d-glucose (18-F-FDG) avidity of the tumor mass after four cycles of treatment with Compound A administered at 200 mg BID to a patient with NSCLC.
  • the patient had received pemetrexed/pembrolizumab, docetaxel, tegafur/gimeracil/oteracil, and carboplatin/ paclitaxel/atezolizumab.
  • Post-Cycle 2 scan showed a 30.4% reduction in the sum of the longest diameters of target lesions compared with baseline. PR was confirmed on subsequent scans
  • phase II assessed in tumor tissue or plasma by a local test, validated according to local regulation at a CLIA-certified USA laboratory or an accredited local laboratory outside of the USA or centrally assessed on tissue or plasma (only if tissue is unavailable or results from tissue are indeterminant) at a Novartis-designated laboratory prior to enrolment.
  • Subject has had major surgery e.g., intra-thoracic, intra-abdominal or intra-pelvic
  • Major surgery e.g., intra-thoracic, intra-abdominal or intra-pelvic
  • Video-assisted thoracic surgery (VATS) and mediastinoscopy will not be counted as major surgery and subject can be enrolled in the study > 1 week after the procedure.
  • Palliative radiotherapy for bone lesions ⁇ 2 weeks prior to randomization is allowed.
  • CMOS central nervous system
  • Stable brain metastasis by this definition should be established prior to randomization and subject must be clinically stable until the first dose of study treatment.
  • Any other medical condition such as active infection, treated or untreated
  • testing for hepatitis B virus (HBV) or hepatitis C virus infection, tuberculosis and/or HIV (by local laboratory) is not mandatory at screening unless if required by local regulations. Any medical condition or prior surgical resection that may affect the absorption of the investigational drug.
  • Participants who do not tolerate one or more of the study drugs can continue to receive the remaining study treatment.

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • Immunology (AREA)
  • Organic Chemistry (AREA)
  • Biochemistry (AREA)
  • Mycology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Biophysics (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Molecular Biology (AREA)
  • Inorganic Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Microbiology (AREA)
  • Genetics & Genomics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

La présente invention concerne une méthode de traitement du cancer du poumon non à petites cellules (NSCLC) qui héberge une mutation KRAS G12C. La méthode consiste à administrer une quantité thérapeutiquement efficace d'inhibiteur de KRAS G12C 1-6-[(4M)-4-(5-chloro-6-méthyl-5 1H-indazol-4-yl)-5-méthyl-3-(1-méthyl-1 H-indazol-5-yl)-1 H-pyrazol-1-yl]-2-azaspiro [3,3] heptan-2-yl}prop-2-en-1-one (composé A), ou un sel, solvate ou hydrate pharmaceutiquement acceptable de celui-ci, une quantité thérapeutiquement efficace de pembrolizumab, une quantité thérapeutiquement efficace de pémétrexed et une quantité thérapeutiquement efficace de thérapie au platine. En particulier, la présente invention concerne une méthode de traitement du NSCLC, le NSCLC exprimant au moins 1 % de PD-L1 selon le score de proportion tumorale (TPS), plus particulièrement le NSCLC exprimant moins de 50 % de PD-L1 selon le score de proportion tumorale (TPS), plus particulièrement le NSCLC exprimant PD-L1 de 1 à 49 % selon le score de proportion tumorale (TPS), encore plus particulièrement le NSCLC exprimant moins de 1 % de PD-L1 selon le score de proportion tumorale (TPS).
PCT/IB2025/090001 2024-03-27 2025-03-27 Inhibiteur de kras g12c destiné à être utilisé dans le traitement du cancer du poumon non à petites cellules Pending WO2025203012A1 (fr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US202463570531P 2024-03-27 2024-03-27
US63/570,531 2024-03-27

Publications (1)

Publication Number Publication Date
WO2025203012A1 true WO2025203012A1 (fr) 2025-10-02

Family

ID=95825373

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/IB2025/090001 Pending WO2025203012A1 (fr) 2024-03-27 2025-03-27 Inhibiteur de kras g12c destiné à être utilisé dans le traitement du cancer du poumon non à petites cellules

Country Status (1)

Country Link
WO (1) WO2025203012A1 (fr)

Citations (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2009114335A2 (fr) 2008-03-12 2009-09-17 Merck & Co., Inc. Protéines de liaison avec pd-1
US8354509B2 (en) 2007-06-18 2013-01-15 Msd Oss B.V. Antibodies to human programmed death receptor PD-1
WO2021124222A1 (fr) 2019-12-20 2021-06-24 Novartis Ag Dérivés de pyrazolyle utiles en tant qu'agents anticancéreux
WO2022089604A1 (fr) 2020-10-30 2022-05-05 Novartis Ag Nouvelles formes cristallines d'un composé inhibiteur de kras g12c
WO2022135346A1 (fr) 2020-12-22 2022-06-30 Novartis Ag Combinaisons pharmaceutiques comprenant un inhibiteur de kras g12c et utilisations d'un inhibiteur de kras g12c pour le traitement de cancers
WO2022269525A1 (fr) 2021-06-23 2022-12-29 Novartis Ag Associations pharmaceutiques comprenant un inhibiteur de kras g12c et leurs utilisations pour le traitement de cancers
WO2023143605A1 (fr) 2022-01-31 2023-08-03 Novartis Ag Procédé de synthèse de dérivés de pyrazolyle utiles en tant qu'agents anticancéreux
WO2023199180A1 (fr) * 2022-04-11 2023-10-19 Novartis Ag Utilisations thérapeutiques d'un inhibiteur de krasg12c
CN116478141B (zh) 2023-06-20 2023-10-24 药康众拓(江苏)医药科技有限公司 氘代kras抑制剂药物及用途

Patent Citations (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8354509B2 (en) 2007-06-18 2013-01-15 Msd Oss B.V. Antibodies to human programmed death receptor PD-1
WO2009114335A2 (fr) 2008-03-12 2009-09-17 Merck & Co., Inc. Protéines de liaison avec pd-1
WO2021124222A1 (fr) 2019-12-20 2021-06-24 Novartis Ag Dérivés de pyrazolyle utiles en tant qu'agents anticancéreux
WO2022089604A1 (fr) 2020-10-30 2022-05-05 Novartis Ag Nouvelles formes cristallines d'un composé inhibiteur de kras g12c
WO2022135346A1 (fr) 2020-12-22 2022-06-30 Novartis Ag Combinaisons pharmaceutiques comprenant un inhibiteur de kras g12c et utilisations d'un inhibiteur de kras g12c pour le traitement de cancers
WO2022269525A1 (fr) 2021-06-23 2022-12-29 Novartis Ag Associations pharmaceutiques comprenant un inhibiteur de kras g12c et leurs utilisations pour le traitement de cancers
WO2023143605A1 (fr) 2022-01-31 2023-08-03 Novartis Ag Procédé de synthèse de dérivés de pyrazolyle utiles en tant qu'agents anticancéreux
WO2023199180A1 (fr) * 2022-04-11 2023-10-19 Novartis Ag Utilisations thérapeutiques d'un inhibiteur de krasg12c
CN116478141B (zh) 2023-06-20 2023-10-24 药康众拓(江苏)医药科技有限公司 氘代kras抑制剂药物及用途

Non-Patent Citations (5)

* Cited by examiner, † Cited by third party
Title
BERGE ET AL.: "Pharmaceutical Salts", J. PHARM. SCI., vol. 66, 1977, pages 1 - 19, XP002675560, DOI: 10.1002/jps.2600660104
CASSIER PHILIPPE ALEXANDRE ET AL: "KontRASt-01 update: Safety and efficacy of JDQ443 in KRAS G12C-mutated solid tumors including non-small cell lung cancer (NSCLC)", 1 June 2023 (2023-06-01), XP093284252, Retrieved from the Internet <URL:https://ascopubs.org/doi/pdfdirect/10.1200/JCO.2023.41.16_suppl.9007> *
FDA: "HIGHLIGHTS OF PRESCRIBING INFORMATION and FULL PRESCRIBING INFORMATION for KEYTRUDA.", 1 October 2023 (2023-10-01), XP093285686, Retrieved from the Internet <URL:https://www.accessdata.fda.gov/drugsatfda_docs/label/2023/125514s139lbl.pdf> *
HAMID, O. ET AL., NEW ENGLAND JOURNAL OF MEDICINE, vol. 369, no. 2, 2013, pages 134 - 44
SEQUIST ET AL., ANN. ONCOL., vol. 22, no. 12, 2011, pages 2616 - 24

Similar Documents

Publication Publication Date Title
US12343344B2 (en) Pharmaceutical combination comprising TNO155 and ribociclib
CN105873440B (zh) 抑制tie2激酶的组合物在制备治疗癌症的药物中的用途
RU2737496C2 (ru) Способы лечения рака
JP7328151B2 (ja) Ｈｅｒ２陽性がんの処置
WO2021262484A1 (fr) Polythérapie pour le traitement du cancer
WO2023199180A1 (fr) Utilisations thérapeutiques d&#39;un inhibiteur de krasg12c
US20180353602A1 (en) Combination of hdac inhibitor and anti-pd-l1 antibody for treatment of cancer
AU2021267213B2 (en) Pharmaceutical combination comprising TNO155 and nazartinib
UA125436C2 (uk) Фармацевтичні комбінації
WO2022090443A1 (fr) Administration et posologie pour une combinaison d&#39;un inhibiteur de bcl-2 et d&#39;un inhibiteur de mcl-1
US20220241294A1 (en) Bisfluoroalkyl-1,4-benzodiazepinone compounds for treating notch-activated breast cancer
US20220288019A1 (en) Methods of treating cancer using a combination of SERD Dosing Regimens
CA2437768A1 (fr) Systemes de distribution de medicaments anti-tumoraux cibles
TWI776451B (zh) Bcl-2/bcl-xl抑制劑之組合及相關用途
US11419862B2 (en) Quinoline derivative for treatment of nasopharyngeal carcinoma
WO2025203012A1 (fr) Inhibiteur de kras g12c destiné à être utilisé dans le traitement du cancer du poumon non à petites cellules
WO2025202971A1 (fr) Inhibiteur de kras g12c destiné à être utilisé dans le traitement du cancer du poumon non à petites cellules
CN117580572A (zh) 用安森司坦和帕博西尼治疗乳腺癌

Legal Events

Date Code Title Description
121 Ep: the epo has been informed by wipo that ep was designated in this application

Ref document number: 25727526

Country of ref document: EP

Kind code of ref document: A1