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MRTX1133
MRTX1133 is an investigational drug that targets the G12D mutation in KRAS dependent cancers. MRTX1133 was in a phase 1/2 clinical trial for the treatment of solid tumors, however the study was terminated in Q1 2025. MRTX1133 is considered to be harmful from direct skin or eye exposure other than transient irritation. It may cause irritation of the respiratory system if inhaled. See also * ACBI3 * Adagrasib * Olomorasib * RMC-9805 * Sotorasib Sotorasib, sold under the brand names Lumakras and Lumykras, is an anti-cancer medication used to treat non-small-cell lung cancer. It targets a specific mutation, G12C, in the protein K-Ras encoded by gene KRAS which is responsible for vario ... References {{antineoplastic-drug-stub Antineoplastic drugs Pyridopyrimidines Pyrrolizidines Fluoroarenes Ethynyl compounds Naphthols Aromatic ethers ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
KRAS
''KRAS'' ( Kirsten rat sarcoma virus) is a gene that provides instructions for making a protein called K-Ras, a part of the RAS/MAPK pathway. The protein relays signals from outside the cell to the cell's nucleus. These signals instruct the cell to grow and divide ( proliferate) or to mature and take on specialized functions ( differentiate). It is called ''KRAS'' because it was first identified as a viral oncogene in the Kirsten RAt Sarcoma virus. The oncogene identified was derived from a cellular genome, so , when found in a cellular genome, is called a proto-oncogene. The K-Ras protein is a GTPase, a class of enzymes which convert the nucleotide guanosine triphosphate (GTP) into guanosine diphosphate (GDP). In this way the K-Ras protein acts like a switch that is turned on and off by the GTP and GDP molecules. To transmit signals, it must be turned on by attaching (binding) to a molecule of GTP. The K-Ras protein is turned off (inactivated) when it converts the GTP to ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
ACBI3
ACBI3 is an experimental anticancer drug which is one of the first examples of a proteolysis targeting chimera or PROTAC. It is a bifunctional molecule with two halves joined by a linker; one half binds to a protein found in various forms of cancer cell called Kirsten rat sarcoma virus or KRAS, while the other half binds E3 ligase which triggers the cell's natural protein degradation mechanisms so that the entire complex is broken down. In early stage testing, it was able to target 13 of the 17 most common mutated forms of KRAS found in cancer cells, allowing selective targeting of a wide range of cancer types. While this particular molecule is still at an early developmental stage and may be unlikely to be approved as a medicine itself, it is an important proof of concept which is likely to lead to the development of a range of related PROTAC type anticancer drugs. See also * Adagrasib * K-Ras(G12C) inhibitor 6 * MRTX1133 * Olomorasib * RMC-9805 * Sotorasib Sotorasib ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Olomorasib
Olomorasib (LY3537982) is an experimental anticancer drug which acts as an inhibitor of the G12C mutant form of Kirsten rat sarcoma virus (KRAS), an oncogene commonly present in several forms of cancer. It is in early stage clinical trials against lung and colorectal cancers and advanced solid tumors. See also * ACBI3 * Adagrasib * Divarasib * MRTX1133 * RMC-9805 * Sotorasib Sotorasib, sold under the brand names Lumakras and Lumykras, is an anti-cancer medication used to treat non-small-cell lung cancer. It targets a specific mutation, G12C, in the protein K-Ras encoded by gene KRAS which is responsible for vario ... References {{reflist Experimental cancer drugs Benzothiophenes Pyrazines Oxazocines Nitriles Fluoroarenes Chloroarenes Amines Carboxamides Cyclic ketones ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
RMC-9805
RMC-9805 is an investigational drug that selectively targets the G12D mutation in KRAS dependent cancers. RMC-9805 functions as molecular glue that forms a non-covalent ligand-mediated protein-protein interaction between cyclophilin A and GTP-bound RAS. Subsequent covalent modification of the mutant Asp12 residue affords selectivity over wild-type RAS. RMC-9805 is currently in a phase 1/1b clinical trial for the treatment of KRAS G12D-mutant solid tumors. Preliminary data indicated that KRAS G12D–mutant PDAC patients dosed at 1200 mg daily or 600 mg twice daily achieved a 30% objective response rate (n = 12) and 80% disease control rate (n = 32). See also * ACBI3 * Adagrasib * MRTX1133 * Olomorasib * Sotorasib Sotorasib, sold under the brand names Lumakras and Lumykras, is an anti-cancer medication used to treat non-small-cell lung cancer. It targets a specific mutation, G12C, in the protein K-Ras encoded by gene KRAS which is responsible for vario ... ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Investigational Drug
The United States Food and Drug Administration's Investigational New Drug (IND) program is the means by which a pharmaceutical company obtains permission to start human clinical trials and to ship an experimental drug across state lines (usually to clinical investigators) before a marketing application for the drug has been approved. Regulations are primarily at . Similar procedures are followed in the European Union, Japan, and Canada due to regulatory harmonization efforts by the International Council for Harmonisation. Types * Research or investigator INDs are non-commercial INDs filed by researchers to study an unapproved drug or to study an approved drug for a new indication or in a new patient population. * Emergency Use INDs, also called compassionate use or single-patient INDs, are filed for emergency use of an unapproved drug when the clinical situation does not allow sufficient time to submit an IND in accordance wit21 CFR §§ 312.23 312.24. These are most commonly ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Adagrasib
Adagrasib, sold under the brand name Krazati, is an anticancer medication used to treat non-small cell lung cancer. Adagrasib is an inhibitor of G12C mutated KRAS GTPase. It is taken by mouth. It is being developed by Mirati Therapeutics. The most common adverse reactions include diarrhea, nausea, fatigue, vomiting, musculoskeletal pain, hepatotoxicity, renal impairment, dyspnea, edema, decreased appetite, cough, pneumonia, dizziness, constipation, abdominal pain, and QTc interval prolongation. The most common laboratory abnormalities include decreased lymphocytes, increased aspartate aminotransferase, decreased sodium, decreased hemoglobin, increased creatinine, decreased albumin, increased alanine aminotransferase, increased lipase, decreased platelets, decreased magnesium, and decreased potassium. It was approved for medical use in the United States in December 2022 for lung cancer and together with Cetuximab in 2024 for colorectal cancer. Medical uses Adagrasib is indi ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Sotorasib
Sotorasib, sold under the brand names Lumakras and Lumykras, is an anti-cancer medication used to treat non-small-cell lung cancer. It targets a specific mutation, G12C, in the protein K-Ras encoded by gene KRAS which is responsible for various forms of cancer. Sotorasib is an inhibitor of the RAS GTPase family. The most common side effects include diarrhea, musculoskeletal pain, nausea, fatigue, liver damage and cough. The most common adverse reactions for sotorasib used in combination with panitumumab include rash, dry skin, diarrhea, stomatitis, fatigue, and musculoskeletal pain. Sotorasib is the first approved targeted therapy for people with tumors with any KRAS mutation, which accounts for approximately 25% of mutations in non-small cell lung cancers. KRAS G12C mutations occur in about 13% of people with non-small cell lung cancers. While KRAS G12 mutations are common in pancreatic cancer, only 1-2% of pancreatic cancer patients have a G12C mutation, limiting the utilit ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Antineoplastic Drugs
Chemotherapy (often abbreviated chemo, sometimes CTX and CTx) is the type of cancer treatment that uses one or more anti-cancer drugs ( chemotherapeutic agents or alkylating agents) in a standard regimen A regimen is a plan, or course of action such as a Diet (nutrition), diet, exercise or medical treatment. A salt#Health effects, low-salt diet is a regimen. A course of penicillin is a regimen, and there are many chemotherapy regimens in the trea .... Chemotherapy may be given with a curative intent (which almost always involves combinations of drugs), or it may aim only to prolong life or to Palliative care, reduce symptoms (Palliative care, palliative chemotherapy). Chemotherapy is one of the major categories of the medical discipline specifically devoted to pharmacotherapy for cancer, which is called ''oncology#Specialties, medical oncology''. The term ''chemotherapy'' now means the non-specific use of intracellular poisons to inhibit mitosis (cell division) or to indu ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
Fluoroarenes
In organic chemistry, an aryl halide (also known as a haloarene) is an aromatic compound in which one or more hydrogen atoms directly bonded to an aromatic ring are replaced by a halide ion (such as fluorine F''−'', chlorine Cl−1,−3,−5, bromine Br−1, or iodine I−). Aryl halides are distinct from haloalkanes (alkyl halides) due to significant differences in their methods of preparation, chemical reactivity, and physical properties. The most common and important members of this class are aryl chlorides, but the group encompasses a wide range of derivatives with diverse applications in organic synthesis, pharmaceuticals, and materials science. Classification according to halide Aryl fluorides Aryl fluorides are used as synthetic intermediates, e.g. for the preparation of pharmaceuticals, pesticides, and liquid crystals. The conversion of diazonium salts is a well established route to aryl fluorides. Thus, anilines are precursors to aryl fluorides. In the classic Schiemann ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
