Therapy Detail
Contact
Missing content? – Request curation!
Request curation for specific Genes, Variants, or PubMed publications.
Have questions, comments, or suggestions? - Let us know!
Email us at : ckbsupport@genomenon.com
| Therapy Name | Zeteletinib |
| Synonyms | |
| Therapy Description |
Zeteletinib (DS-5010) is a multi-kinase inhibitor that inhibits RET and KDR (VEGFR2), which may lead to inhibition of tumor cell growth (Cancer Res 2019;79(13 Suppl):Abstract nr 2199). |
Filtering
- Case insensitive filtering will display rows if any text in any cell matches the filter term
- Use simple literal full or partial string matches
- Separate multiple filter terms with a space. Any order may be used (i. e. a b c and c b a are equivalent )
- Filtering will only apply to rows that are already loaded on the page. Filtering has no impact on query parameters.
- Use quotes to match on a longer phrase with spaces (i.e. "mtor c1483f")
Sorting
- Generally, the default sort order for tables is set to be first column ascending; however, specific tables may set a different default sort order.
- Click on any column header arrows to sort by that column
- Hold down the Shift key and click multiple columns to sort by more than one column. Be sure to set ascending or descending order for a given column before moving on to the next column.
| Drug Name | Trade Name | Synonyms | Drug Classes | Drug Description |
|---|---|---|---|---|
| Zeteletinib | DS5010|DS 5010|BOS172738|BOS-172738|BOS 172738|DS-5010 | RET Inhibitor 53 VEGFR2 Inhibitor 37 | Zeteletinib (DS-5010) is a multi-kinase inhibitor that inhibits RET and KDR (VEGFR2), which may lead to inhibition of tumor cell growth (Cancer Res 2019;79(13 Suppl):Abstract nr 2199). |
Filtering
- Case insensitive filtering will display rows if any text in any cell matches the filter term
- Use simple literal full or partial string matches
- Separate multiple filter terms with a space. Any order may be used (i. e. a b c and c b a are equivalent )
- Filtering will only apply to rows that are already loaded on the page. Filtering has no impact on query parameters.
- Use quotes to match on a longer phrase with spaces (i.e. "mtor c1483f")
Sorting
- Generally, the default sort order for tables is set to be first column ascending; however, specific tables may set a different default sort order.
- Click on any column header arrows to sort by that column
- Hold down the Shift key and click multiple columns to sort by more than one column. Be sure to set ascending or descending order for a given column before moving on to the next column.
| Molecular Profile | Indication/Tumor Type | Response Type | Therapy Name | Approval Status | Evidence Type | Efficacy Evidence | References |
|---|---|---|---|---|---|---|---|
| RET fusion | lung non-small cell carcinoma | sensitive | Zeteletinib | Phase I | Actionable | In a Phase I trial, Zeteletinib (DS-5010) treatment led to an objective response rate (ORR) of 28% (28/101), disease control rate (DCR) of 58% (59/101), median progression-free survival (mPFS) of 7.16 mo, and median duration of response (mDOR) of 11.10 mo in patients with RET-altered advanced solid tumors, with an ORR of 28% (17/61), DCR of 59% (36/61), mPFS of 6.18 mo, and mDOR of 10.17 mo in patients with non-small cell lung cancer harboring a RET fusion (PMID: 40992271; NCT03780517). | 40992271 |
| RET fusion | pancreatic cancer | predicted - sensitive | Zeteletinib | Case Reports/Case Series | Actionable | In a Phase I trial, Zeteletinib (DS-5010) treatment resulted in an objective response rate (ORR) of 33% (18/54) in patients with RET-altered advanced solid tumors including an ORR of 33% (10/30) in non-small cell lung cancer patients harboring a RET fusion, an ORR of 44% (7/16) in patients with medullary thyroid cancer harboring RET mutations, and a partial response in a pancreatic cancer patient (J Clin Oncol 2021 39: 15_suppl, 3008; NCT03780517). | detail... |
| RET G810S | Advanced Solid Tumor | predicted - sensitive | Zeteletinib | Preclinical - Cell culture | Actionable | In a preclinical study, cells expressing RET G810S in the context of KIF5B-RET were sensitive to Zeteletinib (DS-5010) treatment in culture (Cancer Res (2024) 84 (6_Supplement): 5833). | detail... |
| RET mutant | medullary thyroid carcinoma | sensitive | Zeteletinib | Phase I | Actionable | In a Phase I trial, Zeteletinib (DS-5010) treatment led to an objective response rate (ORR) of 28% (28/101), disease control rate (DCR) of 58% (59/101), median progression-free survival (mPFS) of 7.16 mo, and median duration of response (mDOR) of 11.10 mo in patients with RET-altered advanced solid tumors, with an ORR of 30% (8/27, all PR), DCR of 74% (20/27), mPFS of 12.75 mo, and mDOR of 19.15 mo in medullary thyroid cancer patients harboring a RET mutation including M918T (PMID: 40992271; NCT03780517). | 40992271 |
Filtering
- Case insensitive filtering will display rows if any text in any cell matches the filter term
- Use simple literal full or partial string matches
- Separate multiple filter terms with a space. Any order may be used (i. e. a b c and c b a are equivalent )
- Filtering will only apply to rows that are already loaded on the page. Filtering has no impact on query parameters.
- Use quotes to match on a longer phrase with spaces (i.e. "mtor c1483f")
Sorting
- Generally, the default sort order for tables is set to be first column ascending; however, specific tables may set a different default sort order.
- Click on any column header arrows to sort by that column
- Hold down the Shift key and click multiple columns to sort by more than one column. Be sure to set ascending or descending order for a given column before moving on to the next column.
| Clinical Trial | Phase | Therapies | Title | Recruitment Status | Covered Countries | Other Countries |
|---|---|---|---|---|---|---|
| NCT03780517 | Phase I | Zeteletinib | Safety, Efficacy, and Tolerability of BOS172738 in Patients With Advanced Rearranged During Transfection (RET) Gene-Altered Tumors | Completed | USA | FRA | ESP | BEL | 3 |
CKB BOOST