An open-label phase I dose-finding study of APR-246 in hematological malignancies

doi:10.1038/bcj.2016.60

Clinical Trial

. 2016 Jul 15;6(7):e447.

doi: 10.1038/bcj.2016.60.

An open-label phase I dose-finding study of APR-246 in hematological malignancies

S Deneberg¹, H Cherif², V Lazarevic³, P-O Andersson⁴, M von Euler⁵, G Juliusson³, S Lehmann^{1

2}

Affiliations

¹ Karolinska University Hospital, Center of Hematology and Karolinska Institutet, Institution of Medicine, Huddinge, Sweden.
² Department of Medical Sciences, Uppsala University and Uppsala Academic Hospital, Uppsala, Sweden.
³ Department of Hematology, Skane University Hospital, Lund, Sweden.
⁴ Section of Hematology, South Älvsborg Hospital, Borås and Sahlgrenska Academy, Gothenburg, Sweden.
⁵ Aprea AB, Solna, Sweden.

PMID: 27421096
PMCID: PMC5141349
DOI: 10.1038/bcj.2016.60

Free PMC article

Clinical Trial

An open-label phase I dose-finding study of APR-246 in hematological malignancies

S Deneberg et al. Blood Cancer J. 2016.

Free PMC article

. 2016 Jul 15;6(7):e447.

doi: 10.1038/bcj.2016.60.

Authors

S Deneberg¹, H Cherif², V Lazarevic³, P-O Andersson⁴, M von Euler⁵, G Juliusson³, S Lehmann^{1

2}

Affiliations

¹ Karolinska University Hospital, Center of Hematology and Karolinska Institutet, Institution of Medicine, Huddinge, Sweden.
² Department of Medical Sciences, Uppsala University and Uppsala Academic Hospital, Uppsala, Sweden.
³ Department of Hematology, Skane University Hospital, Lund, Sweden.
⁴ Section of Hematology, South Älvsborg Hospital, Borås and Sahlgrenska Academy, Gothenburg, Sweden.
⁵ Aprea AB, Solna, Sweden.

PMID: 27421096
PMCID: PMC5141349
DOI: 10.1038/bcj.2016.60

No abstract available

PubMed Disclaimer

Conflict of interest statement

P-OA, SL: Advisory board APREA AB. MvO: Employment APREA AB. The remaining authors declare no conflict of interest.

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References

1. Vousden KH, Lu X. Live or let die: the cell's response to p53. Nat Rev Cancer 2002; 2: 594–604. - PubMed
1. Duffy MJ, Synnott NC, McGowan PM, Crown J, O'Connor D, Gallagher WM. p53 as a target for the treatment of cancer. Cancer Treat Rev 2014; 40: 1153–1160. - PubMed
1. Lehmann S, Bykov VJ, Ali D, Andren O, Cherif H, Tidefelt U et al. Targeting p53 in vivo: a first-in-human study with p53-targeting compound APR-246 in refractory hematologic malignancies and prostate cancer. J Clin Oncol 2012; 30: 3633–3639. - PubMed
1. Lambert JM, Gorzov P, Veprintsev DB, Soderqvist M, Segerback D, Bergman J et al. PRIMA-1 reactivates mutant p53 by covalent binding to the core domain. Cancer Cell 2009; 15: 376–388. - PubMed
1. Bykov VJ, Issaeva N, Shilov A, Hultcrantz M, Pugacheva E, Chumakov P et al. Restoration of the tumor suppressor function to mutant p53 by a low-molecular-weight compound. Nat Med 2002; 8: 282–288. - PubMed

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[1] Vousden KH, Lu X. Live or let die: the cell's response to p53. Nat Rev Cancer 2002; 2: 594–604. - PubMed

[2] Vousden KH, Lu X. Live or let die: the cell's response to p53. Nat Rev Cancer 2002; 2: 594–604. - PubMed

[3] Duffy MJ, Synnott NC, McGowan PM, Crown J, O'Connor D, Gallagher WM. p53 as a target for the treatment of cancer. Cancer Treat Rev 2014; 40: 1153–1160. - PubMed

[4] Duffy MJ, Synnott NC, McGowan PM, Crown J, O'Connor D, Gallagher WM. p53 as a target for the treatment of cancer. Cancer Treat Rev 2014; 40: 1153–1160. - PubMed

[5] Lehmann S, Bykov VJ, Ali D, Andren O, Cherif H, Tidefelt U et al. Targeting p53 in vivo: a first-in-human study with p53-targeting compound APR-246 in refractory hematologic malignancies and prostate cancer. J Clin Oncol 2012; 30: 3633–3639. - PubMed

[6] Lehmann S, Bykov VJ, Ali D, Andren O, Cherif H, Tidefelt U et al. Targeting p53 in vivo: a first-in-human study with p53-targeting compound APR-246 in refractory hematologic malignancies and prostate cancer. J Clin Oncol 2012; 30: 3633–3639. - PubMed

[7] Lambert JM, Gorzov P, Veprintsev DB, Soderqvist M, Segerback D, Bergman J et al. PRIMA-1 reactivates mutant p53 by covalent binding to the core domain. Cancer Cell 2009; 15: 376–388. - PubMed

[8] Lambert JM, Gorzov P, Veprintsev DB, Soderqvist M, Segerback D, Bergman J et al. PRIMA-1 reactivates mutant p53 by covalent binding to the core domain. Cancer Cell 2009; 15: 376–388. - PubMed

[9] Bykov VJ, Issaeva N, Shilov A, Hultcrantz M, Pugacheva E, Chumakov P et al. Restoration of the tumor suppressor function to mutant p53 by a low-molecular-weight compound. Nat Med 2002; 8: 282–288. - PubMed

[10] Bykov VJ, Issaeva N, Shilov A, Hultcrantz M, Pugacheva E, Chumakov P et al. Restoration of the tumor suppressor function to mutant p53 by a low-molecular-weight compound. Nat Med 2002; 8: 282–288. - PubMed

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An open-label phase I dose-finding study of APR-246 in hematological malignancies

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An open-label phase I dose-finding study of APR-246 in hematological malignancies

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