14 results about "Letrozole" patented technology

This invention discloses the use of letrozole or its pharmaceutically acceptable salts, solvates, or hydrates in the preparation of medicaments for treating lymphoma. Experimental verification has shown that letrozole or its pharmaceutically acceptable salts, solvates, or hydrates can be used to treat lymphoma, particularly diffuse large B-cell lymphoma with c-MYC rearrangements.

The invention discloses application of maca in preparation of a medicine for improving polycystic ovarian syndrome, and belongs to the field of biological medicine. According to the present invention, letrozole and high-fat feed are adopted to induce and construct a polycystic ovarian syndrome mouse model, and experiments such as estrus cycle detection, ovary and uterus morphology observation, sex hormone detection, blood sugar level detection and the like are performed; results show that the maca can effectively improve the rhythm disorder of the estrus cycle, the polycystic ovarian form and the uterine form of the polycystic ovarian syndrome model mouse, correct the reproductive endocrine disorder, recover the normal ovarian ovulation function and relieve the insulin resistance symptom of the polycystic ovarian syndrome model mouse. A new thought is provided for research and development of medicines for treating the polycystic ovarian syndrome, and maca is expected to become a potential candidate medicine for treating the polycystic ovarian syndrome and has a wide application prospect.

The present invention relates to the technical field of fish breeding and discloses a large-scale breeding method for all-female large yellow croaker. The present invention provides a method for inducing sex reversal in genetically female large yellow croaker by feeding them a formula feed containing letrozole, producing pseudo-male fish. The pseudo-male fish are then identified through live marking and screening. The pseudo-male fish are then fertilized with genetically female large yellow croaker to produce all-female fish, thereby achieving large-scale breeding of all-female seedlings. The method has high induction efficiency for inducing female large yellow croaker to pseudo-male fish, does not use androgens, and is safe and simple.

The invention discloses a method for synthesizing an anti-breast cancer drug letrozole analog. The method uses commercial 4-chlorobenzaldehyde as a starting material, and undergoes a multi-component free radical coupling of [1.1.1] propellerane with 4-chlorobenzaldehyde and 1,3-dioxolane under ultraviolet light irradiation, and then hydrolyzes the product under dilute hydrochloric acid to obtain an intermediate bicyclo[1.1.1]pentane (BCP) aldehyde. The aldehyde is then converted into a cyano group, and the hydroxyl group is chlorinated under thionyl chloride conditions. The product is then reacted with 1,2,4-triazole in the presence of potassium carbonate through a one-step S- N The second reaction yields a benzyl triazole compound containing a BCP structure, which is then subjected to a one-step, photopromoted nickel-catalyzed cyanation of the aryl chloride to yield the target product. The present invention utilizes inexpensive raw materials, a short synthesis process, and mild conditions. The resulting target product is expected to become a novel anti-breast cancer drug with enhanced pharmacological activity.

Provided are improved dosing schedules and compositions for the intramuscular administration of compositions containing aromatase inhibitors such as letrozole, for use in treating letrozole-sensitive diseases, conditions or disorders. In the dosing schedules, a first dose of long-acting injectable composition is administered and after a delay period, a second dose of long-acting injectable composition is administered, which provides overlapping dosing periods and improves oestrogen suppression.

This invention relates to the treatment of breast cancer in a subject, and the subject can be either a male or female subject. Including methods of: treating metastatic breast cancer; refractory breast cancer; AR-positive breast cancer; AR-positive refractory breast cancer; AR-positive metastatic breast cancer; AR-positive and ER-positive breast cancer; triple negative breast cancer; advanced breast cancer; breast cancer that has failed selective estrogen receptor modulator (SERM) (tamoxifen, toremifene, raloxifene), gonadotropin-releasing hormone (GnRH) agonist (goserelin), aromatase inhibitor (AI) (letrozole, anastrozole, exemestane), cyclin-dependent kinase 4 / 6 (CDK 4 / 6) inhibitor (palbociclib (Ibrance), ribociclib (Kisqali), lerociclib, abemaciclib (Vorzenio), trilaciclib, lerociclib), mTOR inhibitor (everolimus), trastuzumab (Herceptin, ado-trastuzumab emtansine), pertuzumab (Perjeta), alpelisib (Piqray) (an inhibitor of phosphatidylinositol-3-kinase subunit alpha (PI3Kα)), lapatinib, neratinib (Nerlynx), olaparib (Lynparza) (an inhibitor of the enzyme poly ADP ribose polymerase (PARP)), bevacizumab (Avastin), and / or fulvestrant treatments; metastasis in a subject suffering from breast cancer; HER2-positive; treating a subject suffering from ER mutant expressing breast cancer and / or treating breast cancer in a subject, by first determining the 18F-16β-fluoro-5α-dihydrotestosterone (18F-DHT) tumor uptake and identifying said subject as having AR-positive breast cancer based on 18F-DHT tumor uptake, comprising administering to the subject a therapeutically effective amount of a selective androgen receptor modulator (SARM) compound and a cyclin-dependent kinase 4 / 6 (CDK 4 / 6) inhibitor.

The application provides a composition for treating infertility caused by polycystic ovary syndrome, which is composed of traditional Chinese medicines and western medicines. The traditional Chinese medicines are prepared from raw medicinal materials in the following proportions by weight: 5-13 parts of donkey-hide gelatin, 9-21 parts of prepared rehmannia, 5-13 parts of angelica, 9-21 parts of semen cuscutae, 5-13 parts of ligustrum lucidum ait, 5-13 parts of codonopsis pilosula, 5-13 parts of white atractylodes rhizome, 9-21 parts of polygonatum, 5-13 parts of rhizoma caryophylli, and 5-13 parts of chuanxiong. The western medicine is letrozole. The application also provides the use of the composition. The advantage of the application is that clinical and animal experiments have confirmed that the effect of letrozole combined with the traditional Chinese medicine decoction of the application on treating infertility caused by polycystic ovary syndrome is better, and the ovulation rate and pregnancy rate are significantly improved, so the application is worth promoting.

Provided are combination therapies comprising a PI3K inhibitor (e.g., inavolisib), a CDK4 / 6 inhibitor (e.g., palbociclib), and fulvestrant; and methods of treating hormone receptor positive and HER2 negative (HR+ / HER2−) locally advanced or metastatic breast cancer in a patient (preferably a patient with a PIC3CA mutant patient) comprising administering a therapeutically effective amount of inavolisib, or a pharmaceutically acceptable salt thereof, a CDK4 / 6 inhibitor (e.g., palbociclib), and fulvestrant or letrozole.

The application provides use of CYP2A6 genotype as a marker for predicting the efficacy of neoadjuvant chemotherapy combined with neoadjuvant endocrine therapy for breast cancer, patients with CYP2A6 intermediate / slow metabolism type are more likely to achieve pCR than patients with normal metabolism type, CYP2A6 rs61663607 T>C TT type is more likely to achieve pCR than TC and CC types, in patients with neoadjuvant chemotherapy combined with or without letrozole, CYP2A6 rs7250713 G>C CC type is more likely to achieve pCR than CC and CG types. The application also provides use of CYP2A6 genotype in preparation of a reagent for diagnosing and predicting the efficacy of neoadjuvant chemotherapy combined with neoadjuvant endocrine therapy for breast cancer. The application is used for auxiliary diagnosis of the efficacy of neoadjuvant chemotherapy combined with or without letrozole treatment for early hormone receptor positive breast cancer patients receiving neoadjuvant therapy and surgery.

The application discloses a crystal III type substance of letrozole compound (chemical name: 1-[bis(4-cyanophenyl)methyl]-1,2,4-triazole, English name: Letrozole), a preparation method of the crystal III type substance, and a pharmaceutical composition and application of the crystal III type substance. Specifically, the application discloses a crystal III type solid substance state of the letrozole compound, a preparation method of a crystal III type solid substance sample, and application of the letrozole crystal substance as an active ingredient in preparation of an anti-hormone antitumor drug.

The invention belongs to the field of pharmaceutical preparations, and provides a medicine for treating infertility and a preparation method thereof. According to the invention, a biphase controlled release tablet design is adopted, a quick release layer contains 0.8-2.0 wt% of polyethylene glycol-hemisuccinic acid choline salt as an ion pair auxiliary release agent, and the polyethylene glycol-hemisuccinic acid choline salt has accurately regulated number-average molecular weight of 1000-2000, terminal group substitution degree of 1.8-2.0, neutralization degree of more than or equal to 95% and low acid value of less than or equal to 5.0 mg KOH / g; the surfaces of letrozole particles are micro-coated with a fluidized bed to form 1.0-1.5 wt% of a uniform weight-increasing coating layer, and diffusion control of 15-45 wt% of hydroxypropyl methylcellulose in a slow-release layer is combined, so that double-time-window stable drug release of 45-60% of accumulated release within 2 hours and 85-95% of accumulated release within 24 hours is realized; triple contradictions between tablet densification and double-time window release channel maintenance, micro-coating process window and initial release consistency, low water-containing stability of a formula and ion pair assisted release hydration requirements are solved, and the tablet is suitable for treating ovulation disorder related infertility and has wide clinical application value.

Methods for treating gliomas, such as glioblastoma, including administering an aromatase inhibitor, such as letrozole, to a subject suffering from a glioma. The method may further include administering the aromatase inhibitor in combination with a poly-ADP ribose polymerase inhibitor, such as olaparib, pamiparib, veliparib or niraparib.

The application discloses a crystal II type substance of letrozole compound (chemical name: 1-[bis(4-cyanophenyl)methyl]-1,2,4-triazole, English name: Letrozole), a preparation method of the crystal II type substance, and a pharmaceutical composition and application of the crystal II type substance. Specifically, the application discloses a crystal II type solid substance state of the letrozole compound, a preparation method of a crystal II type solid substance sample, and application of the letrozole crystal substance as an active ingredient in preparation of an anti-hormone antitumor drug.

The invention relates to an induction method and feed for XX type pseudo male fishes of Atlantic salmon and application of the induction method and the feed, and belongs to the technical field of aquaculture breeding, the method comprises the following steps: when genetic female fish fries of Atlantic salmon open mouths for ingestion, 17 alpha-methyltestosterone or letrozole is fed every day, the feeding time duration is greater than or equal to 60 days, and the XX type pseudo male fishes are obtained. The invention also provides a feed containing 17 alpha-methyltestosterone or letrozole and application of the feed to culture of pseudo male Atlantic salmon. According to the invention, the effective window period is accurately shortened to the 60th day from the beginning of exogenous ingestion to ingestion, and the induction success rate of 1.5-4.5 mg / kg of 17 alpha-methyltestosterone can reach 100%; the induction success rate of 150 mg / kg letrozole is 80%, the induction success rate of 200 mg / kg letrozole is 83%, and the induction success rate of 250 mg / kg letrozole is 100%.