Repositioning Candidate Details
| Candidate ID: | R1449 |
| Source ID: | DB12483 |
| Source Type: | approved; investigational |
| Compound Type: | small molecule |
| Compound Name: | Copanlisib |
| Synonyms: | Copanlisib |
| Molecular Formula: | C23H28N8O4 |
| SMILES: | COC1=C(OCCCN2CCOCC2)C=CC2=C1N=C(NC(=O)C1=CN=C(N)N=C1)N1CCN=C21 |
| Structure: |
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| DrugBank Description: | Copanlisib is a selective pan-Class I phosphoinositide 3-kinase (PI3K/Phosphatidylinositol-4,5-bisphosphate 3-kinase/phosphatidylinositide 3-kinase) inhibitor that was first developed by Bayer Healthcare Pharmaceuticals, Inc. The drug targets the enzyme that plays a role in regulating cell growth and survival. Copanlisib was granted accelerated approval on September 14, 2017 under the market name Aliqopa for the treatment of adult patients with relapsed follicular lymphoma and a treatment history of at least two prior systemic therapies. Follicular lymphoma is a slow-growing type of non-Hodgkin lymphoma that is caused by unregulated proliferation and growth of lymphocytes. The active ingredient in Aliquopa intravenous therapy is copanlisib dihydrochloride. |
| CAS Number: | 1032568-63-0 |
| Molecular Weight: | 480.529 |
| DrugBank Indication: | Indicated for the treatment of adult patients with relapsed follicular lymphoma (FL) who have received at least two prior systemic therapies. |
| DrugBank Pharmacology: | Copanlisib has demonstrated potent anti-tumor and pro-apoptotic activity in various tumor cell lines and xenograft models . In clinical trials, 59 percent of patients receiving copanlisib achieved complete or partial shrinkage of their tumors after a median of 12.2 months . Higher systemic levels of copanlisib is associated with elevated plasma glucose levels. |
| DrugBank MoA: | Follicular lymphoma is a B-cell lymphoma that is one of the most common type of non-Hodgkin lymphoma (NHL). It involves unregulated growth and proliferation of lymphocytes that eventually may travel to other organs including the lymph nodes, spleen, and the bone marrow, to form tumors. The phosphatidylinositol 3-kinase (PI3K)-mediated pathway is involved in promoting cell survival proliferation and differentiation however abberant activation of this pathway may lead to tumorigenesis . Copanlisib mediates an inhibitory action on p110α and p110δ isoforms of phosphatidylinositol-3-kinase (PI3K) expressed in malignant B cells. It induces tumor cell death via apoptosis and inhibits the proliferation of primary malignant B cell lines . Copanlisib inhibits several key cell-signaling pathways, including B-cell receptor (BCR) signaling, CXCR12 mediated chemotaxis of malignant B cells, and NFκB signaling in lymphoma cell lines . |
| Targets: | Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform inhibitor; Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform inhibitor |
| Inclusion Criteria: | Therapeutic strategy associated |
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