Therapy Detail
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| Therapy Name | SHP099 |
| Synonyms | |
| Therapy Description |
SHP099 is an allosteric inhibitor of SHP2 that stabilizes SHP2 in its autoinhibited conformation, which reduces downstream signaling and potentially leads to decreased growth of receptor tyrosine kinase-driven tumors (PMID: 27362227, PMID: 31043123). |
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| Drug Name | Trade Name | Synonyms | Drug Classes | Drug Description |
|---|---|---|---|---|
| SHP099 | SHP-099|SHP 099 | SHP2 Inhibitor 20 | SHP099 is an allosteric inhibitor of SHP2 that stabilizes SHP2 in its autoinhibited conformation, which reduces downstream signaling and potentially leads to decreased growth of receptor tyrosine kinase-driven tumors (PMID: 27362227, PMID: 31043123). |
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")
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| Molecular Profile | Indication/Tumor Type | Response Type | Therapy Name | Approval Status | Evidence Type | Efficacy Evidence | References |
|---|---|---|---|---|---|---|---|
| NRAS mutant | hematologic cancer | predicted - resistant | SHP099 | Preclinical | Actionable | In a preclinical study, hematopoietic cancer cell lines harboring NRAS mutations demonstrated resistance to SHP099 in cell culture (PMID: 27362227). | 27362227 |
| FGFR2 M538I | estrogen-receptor positive breast cancer | sensitive | SHP099 | Preclinical - Cell culture | Actionable | In a preclinical study, SHP099 treatment decreased viability of ESR1-positive breast cancer cells expressing FGFR2 M538I in culture (PMID: 32723837). | 32723837 |
| FLT3 exon 14 ins | acute myeloid leukemia | predicted - sensitive | SHP099 | Preclinical - Pdx | Actionable | In a preclinical study, treatment with SHP099 resulted in reduction of CD45-positive leukemic cells and decreased splenomegaly in a human primary tumor-derived xenograft model of acute myeloid leukemia harboring a FLT3-ITD mutation (PMID: 27362227). | 27362227 |
| BRAF V600E | colorectal cancer | resistant | SHP099 | Preclinical - Cell culture | Actionable | In a preclincial study, colorectal cancer cell lines harboring BRAF V600E demonstrated resistance to SHP099 in culture (PMID: 27362227). | 27362227 |
| BRAF V600E | melanoma | no benefit | SHP099 | Preclinical | Actionable | In a preclinical study, SHP099 did not inhibit proliferation or ERK activation in a melanoma cell line harboring BRAF V600E in culture (PMID: 27362227). | 27362227 |
| FGFR2 N550K | estrogen-receptor positive breast cancer | sensitive | SHP099 | Preclinical - Cell culture | Actionable | In a preclinical study, SHP099 treatment decreased viability of ESR1-positive breast cancer cells expressing FGFR2 N550K in culture (PMID: 32723837). | 32723837 |
| NRAS Q61K | neuroblastoma | predicted - resistant | SHP099 | Preclinical - Cell line xenograft | Actionable | In a preclinical study, neuroblastoma cell lines either harboring or expressing NRAS Q61K demonstrated resistance to treatment with SHP099, with increased cell viability and proliferation compared to wild-type Nras in culture, and moderate growth inhibition in cell line xenograft models compared when compared to combination therapies (PMID: 32586982). | 32586982 |
| FGFR2 K660N | estrogen-receptor positive breast cancer | sensitive | SHP099 | Preclinical - Cell culture | Actionable | In a preclinical study, SHP099 treatment decreased viability of ESR1-positive breast cancer cells expressing FGFR2 K660N in culture (PMID: 32723837). | 32723837 |
| ALK R1275Q | neuroblastoma | sensitive | SHP099 | Preclinical - Cell culture | Actionable | In a preclinical study, SHP099 decreased viability of neuroblastoma cell lines harboring ALK R1275Q in culture (PMID: 38032104). | 38032104 |
| JAK2 V617F | hematologic cancer | sensitive | SHP099 | Preclinical - Cell culture | Actionable | In a preclinical study, SHP099 inhibited proliferation of a hematopoietic cancer cell line harboring JAK2 V617F in culture (PMID: 27362227). | 27362227 |
| ALK F1174L | neuroblastoma | sensitive | SHP099 | Preclinical - Cell culture | Actionable | In a preclinical study, SHP099 decreased viability of neuroblastoma cell lines harboring ALK F1174L in culture (PMID: 38032104). | 38032104 |
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| Clinical Trial | Phase | Therapies | Title | Recruitment Status | Covered Countries | Other Countries |
|---|
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