Therapeutical Options in ROS1—Rearranged Advanced Non Small Cell Lung Cancer
ROS proto-oncogene 1 (ROS1) rearrangements occur in 0.9–2.6% of patients with non small cell lung cancer (NSCLC), conferring sensitivity to treatment with specific tyrosine-kinase inhibitors (TKI). Crizotinib, a first-generation TKI, was the first target-therapy approved for the first-line treatment...
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| Format: | Article |
| Language: | English |
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MDPI AG
2023-07-01
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| Series: | International Journal of Molecular Sciences |
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| Online Access: | https://www.mdpi.com/1422-0067/24/14/11495 |
| _version_ | 1797589069637615616 |
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| author | Brigida Stanzione Alessandro Del Conte Elisa Bertoli Elisa De Carlo Alberto Revelant Michele Spina Alessandra Bearz |
| author_facet | Brigida Stanzione Alessandro Del Conte Elisa Bertoli Elisa De Carlo Alberto Revelant Michele Spina Alessandra Bearz |
| author_sort | Brigida Stanzione |
| collection | DOAJ |
| description | ROS proto-oncogene 1 (ROS1) rearrangements occur in 0.9–2.6% of patients with non small cell lung cancer (NSCLC), conferring sensitivity to treatment with specific tyrosine-kinase inhibitors (TKI). Crizotinib, a first-generation TKI, was the first target-therapy approved for the first-line treatment of ROS1-positive NSCLC. Recently, entrectinib, a multitarget inhibitor with an anti-ROS1 activity 40 times more potent than crizotinib and better activity on the central nervous system (CNS), received approval for treatment-naive patients. After a median time-to-progression of 5.5–20 months, resistance mechanisms can occur, leading to tumor progression. Therefore, newer generation TKI with greater potency and brain penetration have been developed and are currently under investigation. This review summarizes the current knowledge on clinicopathological characteristics of ROS1-positive NSCLC and its therapeutic options. |
| first_indexed | 2024-03-11T01:01:06Z |
| format | Article |
| id | doaj.art-d711bbfafc3c4b85a9492091f37ff1a2 |
| institution | Directory Open Access Journal |
| issn | 1661-6596 1422-0067 |
| language | English |
| last_indexed | 2024-03-11T01:01:06Z |
| publishDate | 2023-07-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | International Journal of Molecular Sciences |
| spelling | doaj.art-d711bbfafc3c4b85a9492091f37ff1a22023-11-18T19:40:23ZengMDPI AGInternational Journal of Molecular Sciences1661-65961422-00672023-07-0124141149510.3390/ijms241411495Therapeutical Options in ROS1—Rearranged Advanced Non Small Cell Lung CancerBrigida Stanzione0Alessandro Del Conte1Elisa Bertoli2Elisa De Carlo3Alberto Revelant4Michele Spina5Alessandra Bearz6Department of Medical Oncology, Centro di Riferimento Oncologico di Aviano (CRO), IRCCS, 33081 Aviano, ItalyDepartment of Medical Oncology, Centro di Riferimento Oncologico di Aviano (CRO), IRCCS, 33081 Aviano, ItalyDepartment of Medical Oncology, Centro di Riferimento Oncologico di Aviano (CRO), IRCCS, 33081 Aviano, ItalyDepartment of Medical Oncology, Centro di Riferimento Oncologico di Aviano (CRO), IRCCS, 33081 Aviano, ItalyDepartment of Radiotherapy, Centro di Riferimento Oncologico di Aviano (CRO), IRCCS, 33081 Aviano, ItalyDepartment of Medical Oncology, Centro di Riferimento Oncologico di Aviano (CRO), IRCCS, 33081 Aviano, ItalyDepartment of Medical Oncology, Centro di Riferimento Oncologico di Aviano (CRO), IRCCS, 33081 Aviano, ItalyROS proto-oncogene 1 (ROS1) rearrangements occur in 0.9–2.6% of patients with non small cell lung cancer (NSCLC), conferring sensitivity to treatment with specific tyrosine-kinase inhibitors (TKI). Crizotinib, a first-generation TKI, was the first target-therapy approved for the first-line treatment of ROS1-positive NSCLC. Recently, entrectinib, a multitarget inhibitor with an anti-ROS1 activity 40 times more potent than crizotinib and better activity on the central nervous system (CNS), received approval for treatment-naive patients. After a median time-to-progression of 5.5–20 months, resistance mechanisms can occur, leading to tumor progression. Therefore, newer generation TKI with greater potency and brain penetration have been developed and are currently under investigation. This review summarizes the current knowledge on clinicopathological characteristics of ROS1-positive NSCLC and its therapeutic options.https://www.mdpi.com/1422-0067/24/14/11495ROS1non small cell lung cancertarget therapy |
| spellingShingle | Brigida Stanzione Alessandro Del Conte Elisa Bertoli Elisa De Carlo Alberto Revelant Michele Spina Alessandra Bearz Therapeutical Options in ROS1—Rearranged Advanced Non Small Cell Lung Cancer International Journal of Molecular Sciences ROS1 non small cell lung cancer target therapy |
| title | Therapeutical Options in ROS1—Rearranged Advanced Non Small Cell Lung Cancer |
| title_full | Therapeutical Options in ROS1—Rearranged Advanced Non Small Cell Lung Cancer |
| title_fullStr | Therapeutical Options in ROS1—Rearranged Advanced Non Small Cell Lung Cancer |
| title_full_unstemmed | Therapeutical Options in ROS1—Rearranged Advanced Non Small Cell Lung Cancer |
| title_short | Therapeutical Options in ROS1—Rearranged Advanced Non Small Cell Lung Cancer |
| title_sort | therapeutical options in ros1 rearranged advanced non small cell lung cancer |
| topic | ROS1 non small cell lung cancer target therapy |
| url | https://www.mdpi.com/1422-0067/24/14/11495 |
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