Rebastinib is an investigational, orally administered, potent, and selective inhibitor of the TIE2 kinase, the receptor for angiopoietins, an important family of vascular growth factors. TIE2 has an important role in regulating tumor angiogenesis, invasiveness, metastasis, and immunotolerance. In addition, there is a distinct population of pro-tumoral M2 macrophages in which TIE2 is active, known as TIE2 expressing macrophages (TEMs).

Rebastinib is currently in clinical development for the treatment of multiple solid tumors in combination with chemotherapy in two Phase 1b/2 studies, one with paclitaxel and one with carboplatin.

Tumor TypeStatus
Combo with Paclitaxel
Combo with Carboplatin
Phase 1b/2 Study – Ongoing
Phase 1b/2 Study – Ongoing

Rebastinib in Combination with Paclitaxel

Rebastinib is currently being evaluated in a Phase 1b/2 study in combination with paclitaxel. This is an open-label, multicenter, two-part study to assess safety, tolerability, pharmacokinetics (PK), and efficacy in patients with advanced or metastatic solid tumors.

  • Part 1 of this study was designed to evaluate the safety, tolerability, and PK of two dose cohorts of rebastinib in combination with paclitaxel, and to determine the Phase 2 dose of rebastinib in combination with paclitaxel in patients with advanced or metastatic solid tumors that are refractory to standard therapies.
  • Part 2 of this study was designed to evaluate the safety, tolerability, and efficacy of the Phase 2 dose of rebastinib in combination with weekly paclitaxel across multiple cohorts, including: breast, ovarian, endometrial cancers, and carcinosarcoma.

Part 2 of this study was designed to evaluate the safety, tolerability, and efficacy of the Phase 2 dose of rebastinib in combination with weekly paclitaxel across multiple cohorts, including: breast, ovarian, endometrial cancers, and carcinosarcoma.

We have completed Part 1 of the study and selected a Phase 2 dose of 50 mg twice daily of rebastinib and activated Part 2 of the Phase 1b/2 study of rebastinib in combination with paclitaxel. Data presented from Part 1 of the study demonstrated encouraging preliminary anti-tumor activity, with objective responses seen across a heavily pre-treated patient population, including patients with prior exposure to paclitaxel.

In May 2020, we announced that both the endometrial and ovarian cancer cohorts in Part 2 of the study advanced into the second stage of the Simon two-stage design based on demonstrating at least five responses in each cohort. Data from Part 2 (Stage 1) of the endometrial cancer cohort were presented at the ASCO 2020 Virtual Scientific Program and showed an objective response rate of 39%, confirmed and unconfirmed, and a clinical benefit rate of 72% at eight weeks. In addition, data from Part 2 (Stage 1) of the ovarian cancer cohort was featured at the ESMO Virtual Congress 2020 and showed an objective response rate of 38%, confirmed and unconfirmed, and a clinical benefit rate of 88% at eight weeks.

2020 ESMO Presentation

Most Recent Press Release

Rebastinib in Combination with Carboplatin

A second clinical study of rebastinib is being evaluated in the Phase 1b/2 study in combination with carboplatin. This is an open-label, multicenter, two-part study to assess safety, tolerability, PK, and efficacy in patients with advanced or metastatic solid tumors.

  • Part 1 of this study was designed to evaluate the safety, tolerability, and PK of two dose cohorts of rebastinib in combination with carboplatin, and to determine the Phase 2 dose of rebastinib in combination with carboplatin in patients with advanced or metastatic solid tumors that are refractory to standard therapies.
  • Part 2 of this study was designed to evaluate the safety, tolerability, and efficacy of the Phase 2 dose of rebastinib in combination with carboplatin every three weeks across multiple cohorts, including: breast and ovarian cancers as well as mesothelioma.

We have completed Part 1 of the study and selected a Phase 2 dose of 50 mg twice daily of rebastinib and activated Part 2 of the Phase 1b/2 study of rebastinib in combination with carboplatin. We reported data from Part 1 of the Phase 1b/2 study in combination with carboplatin at ESMO Virtual Congress 2020.

2020 ESMO Presentation

Most Recent Press Release

In addition, further information regarding rebastinib and Deciphera’s pipeline is available in the most recent corporate presentation here »

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