About Chronic Myelogenous Leukemia (CML)
Chronic myeloid leukemia (CML) is also known as chronic myelogenous leukemia.CML is a fairly slow growing leukemia, but it can change into a fast-growing acute leukemia that’s hard to treat. It’s a type of cancer that starts in certain blood-forming cells of the bone marrow.
6 kinds of targeted drugs for the treatment of chronic myeloid leukemia can be made in Laos
- Imatinib
- Dasatinib
- Nilotinib
- Bosutinib
- Ponatinib
- Asciminib
Tyrosine Kinase Inhibitors (TKIs)
Chronic myeloid leukemia (CML) cells contain an abnormal gene, BCR-ABL, that isn’t found in normal cells. This gene makes a protein, BCR-ABL, which causes CML cells to grow and reproduce out of control. BCR-ABL is a type of protein known as a tyrosine kinase. Drugs known as tyrosine kinase inhibitors (TKIs) that target BCR-ABL are the standard treatment for CML.
1、Imatinib
Imatinib was the first drug to specifically target the BCR-ABL tyrosine kinase protein.Almost all CML patients respond to treatment with imatinib, and most of these responses seem to last for many years.Imatinib is taken by mouth as a pill with food, usually once a day.
| Drug Profile | A tyrosine kinase inhibitor and ANTINEOPLASTIC AGENT that inhibits the BCR-ABL kinase created by chromosome rearrangements in CHRONIC MYELOID LEUKEMIA and ACUTE LYMPHOBLASTIC LEUKEMIA, as well as PDG-derived tyrosine kinases that are overexpressed in gastrointestinal stromal tumors. |
| Alternative Names | Imatinib Mesylate – Exvastat; Impentri® |
| Originator | Exvastat |
| Developer | null |
| Class | Amines; Anti-inflammatories; Antineoplastics; Antivirals; Benzamides; Eye disorder therapies; Piperazines; Pyridines; Pyrimidines; Small molecules |
| Mechanism of Action | Angiogenesis inhibitors; Bcr-abl tyrosine kinase inhibitors; Platelet-derived growth factor receptor antagonists; Proto oncogene protein c-kit inhibitors; Signal transduction pathway inhibitors |
| Orphan Drug Status | null |
| Patent Information | There is one patent protecting this compound and two Paragraph IV challenges. |
2、Dasatinib
Dasatinib is another TKI that targets the BCR-ABL protein.This drug is a pill taken once a day with or without food.Dasatinib can be used as the first treatment for CML, but it can also be helpful for patients who can’t take imatinib because of side effects or because imatinib isn’t working.
| Drug Profile | A pyrimidine and thiazole derived ANTINEOPLASTIC AGENT and PROTEIN KINASE INHIBITOR of BCR-ABL KINASE. It is used in the treatment of patients with CHRONIC MYELOID LEUKEMIA who are resistant or intolerant to IMATINIB. |
| Alternative Names | BMS-354825; Sprycel |
| Originator | Bristol-Myers Squibb |
| Developer | Bristol-Myers Squibb; City of Hope National Medical Center; Dana-Farber Cancer Institute; Massachusetts General Hospital; Otsuka Pharmaceutical; Sarcoma Alliance for Research through Collaboration; University of Texas M. D. Anderson Cancer Center; Weill Cornell Medical College |
| Class | Amides; Antineoplastics; Chlorobenzenes; Piperazines; Pyrimidines; Small molecules; Thiazoles |
| Mechanism of Action | Bcr-abl tyrosine kinase inhibitors; EphA2 receptor antagonists; Platelet-derived growth factor beta receptor antagonists; Proto oncogene protein c-kit inhibitors; Src-Family kinase inhibitors |
| Orphan Drug Status | Yes – Chronic myeloid leukaemia; Precursor cell lymphoblastic leukaemia-lymphoma |
| Patent Information | There are two patents protecting this compound and three Paragraph IV challenges. |
3、Nilotinib
Nilotinib is another TKI that targets the BCR-ABL protein. This drug can be used as a first treatment for CML, and is also used for people who can’t take imatinib or whose CML no longer responds to it.It’s taken as a pill. The patient cannot eat 2 hours before taking nilotinib and for 1 hour after taking it.
| Drug Profile | Nilotinib is an inhibitor of the BCR-ABL kinase. Nilotinib binds to and stabilizes the inactive conformation of the kinase domain of ABL protein. In vitro, nilotinib inhibited BCR-ABL mediated proliferation of murine leukemic cell lines and human cell lines derived from patients with Ph+ CML. Under the conditions of the assays, nilotinib was able to overcome imatinib resistance resulting from BCR-ABL kinase mutations, in 32 out of 33 mutations tested. In vivo, nilotinib reduced the tumor size in a murine BCR-ABL xenograft model. |
| Alternative Names | AMN-107; Nilotinib-nanoparticle-formulation-Xspray-Pharma; RightSize-nilotinib; Tasigna |
| Originator | Novartis Pharmaceuticals Corporation |
| Developer | Centre Hospitalier Univeristaire De Lille; Dana-Farber Cancer Institute; Hospital for Special Surgery; Novartis Pharmaceuticals Corporation; Seoul St. Mary’s Hospital; University Health Network of Toronto; University of California, San Diego |
| Class | Antineoplastics; Benzamides; Fluorinated hydrocarbons; Imidazoles; Ketones; Pyridines; Pyrimidines; Small molecules |
| Mechanism of Action | Bcr-abl tyrosine kinase inhibitors; Platelet derived growth factor alpha receptor antagonists; Platelet-derived growth factor beta receptor antagonists; Proto oncogene protein c-kit inhibitors |
| Orphan Drug Status | Yes – Chronic myeloid leukaemia; Precursor cell lymphoblastic leukaemia-lymphoma; Gastrointestinal stromal tumours |
| Patent Information | There are seven patents protecting this compound and one Paragraph IV challenge. |
4、Bosutinib
Bosutinib is another TKI that targets the BCR-ABL protein. It can be used as the first treatment for CML, but most often it’s used if another TKI is no longer working.This drug is taken as a pill with food once a day.
| Drug Profile | a 4-anilino-3-quinolinecarbonitrile dual inhibitor of Src and Abl kinases |
| Alternative Names | Bosulif; PF-05208763; PF-5208763; SKI-606 |
| Originator | Wyeth |
| Developer | Avillion; Massachusetts General Hospital; Pfizer; University of Texas M. D. Anderson Cancer Center |
| Class | Aniline compounds; Antineoplastics; Nitriles; Piperazines; Quinolines; Small molecules; Urologics |
| Mechanism of Action | Bcr-abl tyrosine kinase inhibitors; Src-Family kinase inhibitors |
| Orphan Drug Status | Yes – Chronic myeloid leukaemia |
| Patent Information | There are five patents protecting this compound and two Paragraph IV challenges. |
5、Ponatinib
Ponatinib is a TKI targeting the BCR-ABL protein. Because this drug can cause some serious side effects, it’s only used to treat patients with CML if all of the other TKIs don’t work or if their leukemia cells have a gene change called the T315I mutation. Ponatinib is one TKI to work against CML cells that have this mutation.
This drug is a pill taken once a day with or without food.
| Drug Profile | a pan-Bcr-Abl protein kinase Inhibitor |
| Alternative Names | AP-24534; AP24534 HCl; AP24534 hydrochloride; AP24534-HCL; Iclusig; Ponatinib hydrochloride |
| Originator | ARIAD Pharmaceuticals |
| Developer | Dana-Farber Cancer Institute; Fundacion CRIS de Investigacion para Vencer el Cancer; Incyte Corporation; Massachusetts General Hospital; Mayo Clinic; National Cancer Institute (USA); Otsuka Beijing Research Institute; Otsuka Pharmaceutical; Takeda; University of Birmingham; University of Colorado at Denver |
| Class | Antineoplastics; Benzamides; Imidazoles; Piperazines; Pyridazines; Small molecules |
| Mechanism of Action | Bcr-abl tyrosine kinase inhibitors; Fibroblast growth factor receptor antagonists; Fms-like tyrosine kinase 3 inhibitors; Platelet derived growth factor alpha receptor antagonists; Proto oncogene protein c ret inhibitors; Proto oncogene protein c-kit inhibitors; Vascular endothelial growth factor receptor antagonists |
| Orphan Drug Status | Yes – Precursor cell lymphoblastic leukaemia-lymphoma; Chronic myeloid leukaemia |
| Patent Information | There are five patents protecting this compound. |
6、Asciminib
Asciminib is a TKI targeting a very specific area of the BCR-ABL protein. This drug is used to treat patients with chronic phase CML if two or more other TKIs have already been tried or if their leukemia cells have a gene change called the T315I mutation. Asciminib is another TKI to work against CML cells that have the T315I mutation.This drug is a pill taken once a day or twice a day depending on the dose.
| Drug Profile | Asciminib is an ABL/BCR-ABL1 tyrosine kinase inhibitor. Asciminib inhibits the ABL1 kinase activity of the BCRABL1 fusion protein, by binding to the ABL myristoyl pocket. In studies conducted in vitro or in animal models of CML, asciminib showed activity against wild-type BCR-ABL1 and several mutant forms of the kinase, including the T315I mutation. |
| Alternative Names | ABL 001; ABL-001 – Novartis; Asciminib hydrochloride – Novartis; Scemblix; STAMP inhibitor – Novartis |
| Originator | Novartis |
| Developer | Amides; Antineoplastics; Chlorinated hydrocarbons; Fluorinated hydrocarbons; Phenyl ethers; Pyrazoles; Pyridines; Pyrrolidines; Small molecules |
| Class | Antineoplastics; Benzamides; Imidazoles; Piperazines; Pyridazines; Small molecules |
| Mechanism of Action | Bcr-abl tyrosine kinase inhibitors |
| Orphan Drug Status | Yes – Chronic myeloid leukaemia |
| Patent Information | There is one patent protecting this compound. |
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The WTO’s Council for Trade-Related Aspects of Intellectual Property Rights (TRIPS) ：Under this license, the Lao pharmaceutical industry, as well as the pharmaceutical industry in similar countries（Bangladesh, Nepal, etc.）, will be able to manufacture many drugs without patent authorization.
Reference：
《WTO members agree to extend drug patent exemption for poorest members》https://www.wto.org/english/news_e/news15_e/trip_06nov15_e.htm
《Product Patent Protection,the TRIPS LDC Exemption and the Bangladesh Pharmaceutical Industry》https://www.twn.my/title2/IPR/pdf/ipr17.pdf
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