Obatoclax: Difference between revisions

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{{Chembox
| ImageFile  = Obatoclax.svg
| ImageSize  = 200px
| IUPACName  = 2-(2-((3,5-Dimethyl-1''H''-pyrrol-2-yl)methylene)-3-methoxy-2''H''-pyrrol-5-yl)-1''H''-indole
| OtherNames  = GX15-070
| Section1 = {{Chembox Identifiers
| UNII_Ref      = {{fdacite|correct|FDA}}
| UNII          = QN4128B52A
| CASNo        = 803712-67-6
| CASNo_Ref    = {{cascite|correct|CAS}}
| CASNo1        = 803712-79-0
| CASNo1_Comment = ([[mesylate]])
| CASNo1_Ref    = {{cascite|correct|CAS}}
| PubChem      = 11404337
| PubChem1      = 16681698
| PubChem1_Comment = ([[mesylate]])
| ChemSpiderID  = 24539359
| SMILES        = Cc1cc([nH]c1/C=C/2\C(=CC(=N2)c3cc4ccccc4[nH]3)OC)C
| InChI        = 1S/C20H19N3O/c1-12-8-13(2)21-16(12)10-19-20(24-3)11-18(23-19)17-9-14-6-4-5-7-15(14)22-17/h4-11,21-22H,1-3H3/b19-10+
}}
| Section2 = {{Chembox Properties
| C = 20 | H = 19 | N = 3 | O = 1
| Appearance  = Not available
| Density      = Not available
| MeltingPt    = Not available
| BoilingPt    = Not available
| Solubility  = Not available
}}
| Section3 = {{Chembox Hazards
| MainHazards    = Investigational use only
| FlashPt        = Not applicable
| AutoignitionPt  = Not applicable
}}
| Section5 = {{Chembox Pharmacology
| AdminRoutes    = Intravenous
| Bioavail        = Not well established
| Metabolism      = Hepatic (cytochrome P450 involvement suspected)
| HalfLife        = Short; varies by individual and dosage
| ProteinBound    = Not fully determined
| Excretion      = Likely hepatic/renal pathways
| Legal_status    = Investigational
| Legal_US        = Investigational New Drug
| Legal_UK        = Unlicensed
| Legal_AU        = Not approved
| Legal_CA        = Not approved
| PregCat        = Not assigned
| PregCat_AU      = Not available
| PregCat_US      = Not assigned
}}
}}
'''Obatoclax mesylate''', also known as '''GX15-070''', is an experimental small molecule drug designed to promote [[apoptosis]] (programmed cell death) in cancer cells by acting as a [[Bcl-2 family]] protein antagonist. It was developed by Gemin X Biotechnologies and later acquired by [[Cephalon]], which itself was acquired by [[Teva Pharmaceutical Industries]].
'''Obatoclax mesylate''', also known as '''GX15-070''', is an experimental small molecule drug designed to promote [[apoptosis]] (programmed cell death) in cancer cells by acting as a [[Bcl-2 family]] protein antagonist. It was developed by Gemin X Biotechnologies and later acquired by [[Cephalon]], which itself was acquired by [[Teva Pharmaceutical Industries]].



Latest revision as of 23:25, 2 April 2025

Obatoclax mesylate, also known as GX15-070, is an experimental small molecule drug designed to promote apoptosis (programmed cell death) in cancer cells by acting as a Bcl-2 family protein antagonist. It was developed by Gemin X Biotechnologies and later acquired by Cephalon, which itself was acquired by Teva Pharmaceutical Industries.

Mechanism of Action[edit]

Obatoclax is a pan-inhibitor of the anti-apoptotic Bcl-2 protein family, which includes Bcl-2, Bcl-xL, and Mcl-1. These proteins help cancer cells evade apoptosis. By binding to these proteins, obatoclax restores apoptotic pathways in cancerous cells, potentially enabling effective treatment of hematologic malignancies and solid tumors.

Clinical Development[edit]

Obatoclax mesylate has been evaluated in multiple phase I and phase II clinical trials for cancers such as:

Despite promising preclinical results, clinical outcomes have been limited due to toxicity, particularly neurotoxicity, and modest therapeutic efficacy. Research is ongoing to understand its full potential in combination therapies.

Side Effects[edit]

The most commonly reported adverse effects include:

Status[edit]

As of now, obatoclax is an investigational agent and has not been approved for general clinical use in any country. It continues to be explored in research settings, especially in combination with other chemotherapeutic or targeted agents.

See also[edit]

External links[edit]