Epacadostat(INCB024360) powder video
Epacadostat(INCB024360) powder Characters
|Melt Point:||151–153 °C|
|Storage Temp:||-20°C Freezer|
|Color:||White to off-white powder|
Epacadostat(INCB024360) powder in usage
Epacadostat powder; IDO inhibitor 1; INCB 024360; 1204669-58-8; 1204669-37-3 INCB-024360
Epacadostat powder Usage
Epacadostat powder is an orally available hydroxyamidine and inhibitor of indoleamine 2,3-dioxygenase (IDO1), with potential immunomodulating and antineoplastic activities. Epacadostat powder targets and binds to IDO1, an enzyme responsible for the oxidation of tryptophan into kynurenine. By inhibiting IDO1 and decreasing kynurenine in tumor cells, INCB024360 increases and restores the proliferation and activation of various immune cells, including dendritic cells (DCs), NK cells, and T-lymphocytes, as well as interferon (IFN) production, and a reduction in tumor-associated regulatory T cells (Tregs). Activation of the immune system, which is suppressed in many cancers, may inhibit the growth of IDO1-expressing tumor cells. IDO1 is overexpressed by a variety of tumor cell types and DCs.
INCB024360 powder has been used in trials studying the treatment of HL, Melanoma, Glioblastoma, Mucosal Melanoma, and Ovarian Carcinoma, among others.
Warning on INCB024360 powder
The data lend credence to Incyte’s belief in the mechanism of action of Epacadostat powder. Tumors upregulate the IDO1 enzyme to evade the immune system. Epacadostat powder inhibits this enzyme to dial down this evasion, helping the immune system to hit the tumor with its full force. While more data are needed to confirm the hypothesis, that could have implications for the tussle for the immuno-oncology market.
Incyte’s data stack up well against the combination of Bristol-Myers’ Opdivo and Yervoy, which won FDA approval at the start of last year on the strength of a PFS of 11.5 months in patients with advanced melanoma.
There are reasons to think the slight difference between the PFS results from the clinical trials will ultimately translate into an edge for Incyte. Bristol-Myers’ trial enrolled treatment-naive patients, whereas some subjects in the Incyte study have previously been treated. Incyte’s treatment-naive subpopulation is yet to reach a median PFS but the rates achieved at six, 12 and 18 months suggest it is on track to better the Opdivo-Yervoy result.
Incyte can also point to safety data to argue its combination could better that of Bristol-Myers. The latest update reported 17% of patients suffered grade three or worse treatment-related adverse events. That compares favorably to results generated by Bristol-Myers’ combination, which, in an update earlier this year, was linked to a 58% rate of grade three or four adverse events.
Epacadostat powder is an inhibitor of indoleamine 2,3-dioxygenase 1 (IDO1) with an IC50 value of 7.1 nM in HeLa cells that demonstrates little activity against the related enzymes IDO2 or tryptophan 2,3-dioxygenase (TDO).1 It has been shown to promote T and natural killer-cell growth, to increase IFN-γ production, and to reduce conversion to regulatory T (Treg)-like cells in a coculture system of human allogeneic lymphocytes with either dendritic cells or tumor cells.1 Epacadostat powder can also inhibit tumor growth in tumor-bearing mice in a lymphocyte-dependent manner.
An orally available hydroxyamidine and inhibitor of indoleamine 2,3-dioxygenase (IDO1), with potential immunomodulating and antineoplastic activities. INCB024360 powder targets and binds to IDO1, an enzyme responsible for the oxidation of tryptophan into kynurenine. By inhibiting IDO1 and decreasing kynurenine in tumor cells, Epacadostat powder increases and restores the proliferation and activation of various immune cells, including dendritic cells (DCs), NK cells, and T-lymphocytes, as well as interferon (IFN) production, and a reduction in tumor-associated regulatory T cells (Tregs). Activation of the immune system, which is suppressed in many cancers, may inhibit the growth of IDO1-expressing tumor cells. IDO1 is overexpressed by a variety of tumor cell types and DCs. Check for active clinical trials using this agent.
Indoleamine 2,3-dioxygenase 1 (IDO1) is a key immunosuppressive enzyme that modulates the anti-tumor immune response by promoting regulatory T cell generation and blocking effector T cell activation, thereby facilitating tumor growth by allowing cancer cells to avoid immune surveillance. Epacadostat powder is an investigational, highly potent and selective oral inhibitor of the IDO1 enzyme that regulates the tumor immune microenvironment, thereby restoring effective anti-tumor immune responses. In single-arm studies, the combination of INCB024360 powder and immune checkpoint inhibitors has shown proof-of-concept in patients with unresectable or metastatic melanoma. In these studies, INCB024360 powder combined with the CTLA-4 inhibitor ipilimumab or the PD-1 inhibitor KEYTRUDA improved response rates compared with studies of the immune checkpoint inhibitors alone.
Combining the IDO inhibitor Epacadostat powder with nivolumab (Opdivo) demonstrated promising signs of activity for patients with squamous cell carcinoma of the head and neck (SCCHC) and those with melanoma, according to findings from the phase I/II ECHO-204 study presented at the 2017 ASCO Annual Meeting.
The combination demonstrated an objective response rate (ORR) of 63% and a complete response (CR) rate of 5% for patients with treatment-naive melanoma, in the multi-arm, open-label trial. In those with SCCHC, the ORR was 23% and the CR rate was 3%. The combination was not effective in unselected patients with ovarian cancer and colorectal cancer (CRC).
“INCB024360 powder plus nivolumab was active in phase II melanoma and squamous cell carcinoma of the head and neck cohorts,” said study coauthor Karl D. Lewis, MD, associate professor, Division of Medical Oncology, University of Colorado Anschutz Medical Campus. “Response was observed regardless of PD-L1 expression and HPV status. All responses were ongoing at data cutoff.”
In the phase I portion of the study, the Epacadostat powder dose was escalated from 25 mg twice daily to 300 mg twice daily. In the phase II portion, patients received a 100 mg twice daily and 300 mg twice daily dose of Epacadostat powder. Nivolumab was originally administered at 3 mg/kg every 2 weeks, which was switched to 240 mg IV every 2 weeks in the phase II portion of the study. The findings presented at ASCO for safety were from both portions of the study while the efficacy findings were from just the phase II cohort.
For patients with untreated melanoma (N = 40), the ORR with the 100-mg dose (n = 6) of INCB024360 powder was 100%, which consisted entirely of partial responses. With the 300-mg dose (n = 34), the ORR was 56% and the CR rate was 6%. The disease control rate (DCR; ORR plus stable disease) was 85%. In those with PD-L1–positive tumors (n = 7), the ORR was 71% versus 29% in the PD-L1–negative group (n = 7). All responses were ongoing, with a median duration of 16+ weeks.
In the SCCHN group, in which patients had received ≤2 prior lines of therapy, the ORR with the 100-mg dose (n = 7) of Epacadostat powder was 14%, there were no CRs, and the DCR was 61%. In the 300-mg arm (n = 24), the ORR was 25%, with 1 CR and a DCR of 71%. Patients with PD-L1–positive tumors (n = 10) had an ORR of 30% and those with negative tumors (n = 8) had an ORR of 13%. All responses were ongoing at the analysis, with a median greater than 24+ weeks.
In 29 evaluable patients with ovarian cancer, the ORR was 14% and the DCR was 31%. There was 1 CR in a patient with treatment naive, BRCA-negative, PD-L1–positive disease. In 26 patients with CRC, those with microsatellite instability (MSI) had an ORR of 25% and those with microsatellite stable disease did not experience a response.
“INCB024360 powder plus nivolumab did not demonstrate an efficacy signal in the unselected populations of refractory ovarian cancer and CRC patients,” Lewis said of the results. Regarding future investigations, he noted that the “preliminary safety and efficacy results support further investigation of nivolumab and Epacadostat powder in treatment-naive patients with melanoma and in patients with SCCHN.”
Epacadostat Raw Powder
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