Drugs / Obatoclax
last change Jan 2018 re-read 2 minutes ago

Obatoclax

Small molecule targets BCL2, BCL2A1, BCL2L1, BCL2L10, BCL2L2-PABPN1, MCL1 via inhibition

Developed for
mantle cell lymphoma · small cell lung carcinoma · B-cell chronic lymphocytic leukemia · Hodgkins lymphoma · acute myeloid leukemia · acute undifferentiated leukemia · anaplastic large cell lymphoma · angioimmunoblastic T-cell lymphoma
+29 more · blast phase chronic myelogenous leukemia, BCR-ABL1 positive · Burkitt lymphoma · childhood acute lymphoblastic leukemia · childhood acute myeloid leukemia · chronic lymphocytic leukemia/small lymphocytic lymphoma · diffuse large B-cell lymphoma · extranodal nasal NK/T cell lymphoma · follicular lymphoma · grade III lymphomatoid granulomatosis · hairy cell leukemia · hematopoietic and lymphoid cell neoplasm · hepatosplenic T-cell lymphoma · intraocular lymphoma · large-cell immunoblastic lymphoma · lung cancer · MALT lymphoma · marginal zone lymphoma · metastatic melanoma · mycosis fungoides and variants · myelodysplastic syndrome · myelofibrosis · nodal marginal zone B-cell lymphoma · peripheral T-cell lymphoma, not otherwise specified · plasma cell myeloma · primary cutaneous B-cell lymphoma · primary cutaneous T-cell non-Hodgkin lymphoma · small intestine lymphoma · splenic marginal zone lymphoma · systemic mastocytosis
Investigated by
Gemin X · National Cancer Institute (NCI) · Cephalon · M.D. Anderson Cancer Center

Trials 19 · a red edge is where a trial was stopped

PhaseRegistry idDatesIndicationSponsorStatusOutcome
Phase 15 trials
Phase 1 NCT00933985 Jun 2009 → Apr 2013 Burkitt lymphoma, Hodgkins lymphoma, acute undifferentiated leukemia, anaplastic large cell lymphoma +15 National Cancer Institute (NCI) Terminated No outcome recorded
Phase 1 NCT00612612 Jan 2008 → Jul 2013 B-cell chronic lymphocytic leukemia, prolymphocytic leukemia National Cancer Institute (NCI) Terminated No outcome recorded
Phase 1 NCT00538187 Dec 2007 → Apr 2011 chronic lymphocytic leukemia/small lymphocytic lymphoma, diffuse large B-cell lymphoma, mantle cell lymphoma, marginal zone lymphoma National Cancer Institute (NCI) Terminated No outcome recorded
Phase 1 NCT00438178 Oct 2005 → Oct 2007 hematopoietic and lymphoid cell neoplasm Gemin X Completed No outcome recorded
Phase 1 NCT00600964 Sep 2004 → Jan 2006 B-cell chronic lymphocytic leukemia Gemin X Completed No outcome recorded
Phase 1/27 trials
Phase 1/2 NCT01238146 Oct 2010 → Apr 2012 MALT lymphoma, mantle cell lymphoma, nodal marginal zone B-cell lymphoma, splenic marginal zone lymphoma National Cancer Institute (NCI) Withdrawn No outcome recorded
Phase 1/2 NCT00719901 Jul 2008 → Apr 2011 plasma cell myeloma National Cancer Institute (NCI) Terminated No outcome recorded
Phase 1/2 NCT00724841 Jun → Jul 2008 metastatic melanoma Gemin X Terminated No outcome recorded
Phase 1/2 NCT00682981 May 2008 → Nov 2011 small cell lung carcinoma Gemin X Completed No outcome recorded
Phase 1/2 NCT00521144 Aug 2007 → Aug 2010 small cell lung carcinoma National Cancer Institute (NCI) Completed No outcome recorded
Phase 1/2 NCT00407303 Oct 2006 → Mar 2009 mantle cell lymphoma Gemin X Completed No outcome recorded
Phase 1/2 NCT00405951 Oct 2006 → Nov 2008 lung cancer Gemin X Completed No outcome recorded
Phase 26 trials
Phase 2 NCT00918931 Jun 2009 → Oct 2010 leukemia, systemic mastocytosis M.D. Anderson Cancer Center Terminated No outcome recorded
Phase 2 NCT00684918 Apr 2008 → Aug 2009 acute myeloid leukemia Gemin X Completed No outcome recorded
Phase 2 NCT00427856 Mar 2007 → Feb 2009 follicular lymphoma Gemin X Completed No outcome recorded
Phase 2 NCT00413114 Dec 2006 → Feb 2009 myelodysplastic syndrome Gemin X Completed No outcome recorded
Phase 2 NCT00360035 Jul 2006 → Mar 2008 myelofibrosis Gemin X Completed No outcome recorded
Phase 2 NCT00359892 Jul 2006 → Sep 2007 Hodgkins lymphoma Gemin X Completed No outcome recorded
Phase 31 trial
Phase 3 NCT01563601 Aug 2012 → May 2016 small cell lung carcinoma Cephalon Withdrawn No outcome recorded

Evidence & citations 15 cited values

Every value below carries the sentence it was read from. 24 sources stand behind the page.

FieldValueCited text
Known as Obatoclax Obatoclax was administered to patients with advanced CLL at doses ranging from 3.5 to 14 mg/m(2) as a 1-hour infusion and from 20 to 40 mg/m(2) as a 3-hour infusion every 3 weeks.” PMID 18931344 Oct 2008
17

NCT00684918

NCT00438178

NCT00427856

NCT00359892

NCT00407303

NCT00538187

NCT00612612

NCT00724841

NCT00521144

NCT00933985

NCT00719901

NCT00405951

NCT01563601

NCT00918931

NCT00682981

NCT00360035

NCT00413114

Known as GX15-070 “Phase I study of obatoclax mesylate (GX15-070), a small molecule pan-Bcl-2 family antagonist, in patients with advanced chronic lymphocytic leukemia.” PMID 18931344 Oct 2008
Known as GX15-070MS “Safety and Efficacy of Obatoclax Mesylate (GX15-070MS)in Combination With Docetaxel” NCT00405951
4

“Obatoclax mesylate (GX15-070MS)” NCT00360035

“Obatoclax mesylate (GX15-070MS)” NCT00359892

“Obatoclax mesylate (GX15-070MS)” NCT00413114

“Obatoclax mesylate (GX15-070MS)” NCT00438178

Known as Obatoclax mesilate ChEMBL registry synonym — accepted as the source's own label CHEMBL408194
Known as Obatoclax Mesylate “A Multicenter, Open-Label, 2-Stage, Phase II Study of Single-Agent Obatoclax Mesylate Administered For Three Consecutive Days Every 2 Weeks to Older Patients With Previously...” NCT00684918
13

“A Phase 1 Study of Obatoclax Mesylate (GX15-070MS) in Combination With Fludarabine-Based Chemoimmunotherapy in Previously Treated Patients With B-Cell Chronic Lymphocytic...” NCT00612612

“Phase I study of obatoclax mesylate (GX15-070), a small molecule pan-Bcl-2 family antagonist, in patients with advanced chronic lymphocytic leukemia.” PMID 18931344 Oct 2008

“BACKGROUND: Obatoclax mesylate is a small-molecule Bcl-2 homology domain-3 mimetic that neutralizes antiapoptotic Bcl-2-related proteins.” PMID 25052051 Jun 2014

Obatoclax Mesylate (GMX1777) is a water-soluble, intravenously-administered pro-drug of GMX1778.” NCT00724841

“Patients receive obatoclax mesylate IV over 3 hours and bortezomib IV on days 1, 4, 8, and 11.” NCT00719901

“obatoclax (obatoclax mesylate) administered as a single agent” NCT00933985

obatoclax mesylate, a small-molecule Bcl-2 inhibitor” PMID 24997137 May 2014

obatoclax mesylate, a Bcl-2 antagonist” PMID 21620511 May 2011

Obatoclax mesylate (GX15-070MS)” NCT00360035

Obatoclax mesylate (GX15-070MS)” NCT00359892

Obatoclax mesylate (GX15-070MS)” NCT00438178

“Drug: Obatoclax mesylateNCT00407303

NCT01238146

Known as Obatoclax: CEP-41601 Obatoclax: CEP-41601NCT01563601
Action Inhibit “Obatoclax is designed to restore apoptosis through inhibition of the Bcl-2 family of proteins” NCT00359892
5

“Induced myeloid leukemia cell differentiation protein Mcl-1 inhibitor” CHEMBL408194

“Apoptosis regulator Bcl-W inhibitor” CHEMBL408194

“Apoptosis regulator Bcl-X inhibitor” CHEMBL408194

“Bcl-2-related protein A1 inhibitor” CHEMBL408194

“Bcl-2-like protein 10 inhibitor” CHEMBL408194

Modality Small molecule “a small molecule pan-Bcl-2 family antagonist” PMID 22383790 Mar 2012
Route Intravenous “administered as a 24-hour infusion every 2 weeks” NCT00360035
Target BCL2 “through inhibition of the Bcl-2 family of proteins” NCT00360035
Target BCL2A1 “Bcl-2-related protein A1 inhibitor” CHEMBL408194
Target BCL2L1 “Apoptosis regulator Bcl-X inhibitor” CHEMBL408194
Target BCL2L10 “Bcl-2-like protein 10 inhibitor” CHEMBL408194
Target BCL2L2-PABPN1 “Apoptosis regulator Bcl-W inhibitor” CHEMBL408194
Target MCL1 “Induced myeloid leukemia cell differentiation protein Mcl-1 inhibitor” CHEMBL408194