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Calithera Biosciences
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343 Oyster Point Blvd, Suite 200 South San Francisco, CA 94080
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+1 650 870 1000
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NRF2 mutations are found across multiple solid tumor types, with these mutations occurring in approximately 15% of sqNSCLC patients. CB-228 (sapanisertib) targets a key survival mechanism in NRF2-mutated tumor cells.


Lead Product(s): Sapanisertib

Therapeutic Area: Oncology Product Name: CB-228

Highest Development Status: Phase IIProduct Type: Small molecule

Partner/Sponsor/Collaborator: Not Applicable

Deal Size: Not Applicable Upfront Cash: Not Applicable

Deal Type: Not Applicable October 03, 2022

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MLN0128 (sapanisertib) is an orally bioavailable inhibitor of raptor-mTOR and rictor-mTOR with potential antineoplastic activity, binds to and inhibits both TORC1 and TORC2 complexes of mTOR, which may result in tumor cell apoptosis and a decrease in tumor cell proliferation.


Lead Product(s): Sapanisertib,Telaglenastat Hydrochloride

Therapeutic Area: Oncology Product Name: MLN0128

Highest Development Status: Phase IProduct Type: Small molecule

Partner/Sponsor/Collaborator: Not Applicable

Deal Size: Not Applicable Upfront Cash: Not Applicable

Deal Type: Not Applicable July 13, 2022

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Sapanisertib (CB-228), is a potent and selective, dual mTORC 1/2 inhibitor that targets a key survival mechanism in tumors harboring these mutations in patients with NRF2 -mutated squamous non-small cell lung cancer.


Lead Product(s): Sapanisertib

Therapeutic Area: Oncology Product Name: CB-228

Highest Development Status: Phase IIProduct Type: Small molecule

Partner/Sponsor/Collaborator: Not Applicable

Deal Size: Not Applicable Upfront Cash: Not Applicable

Deal Type: Not Applicable July 06, 2022

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In a retrospective analysis of prior phase 1/2 studies in patients with DLBCL, patients with non-GCB DLBCL who received CB-659 (mivavotinib) had a response rate of 53%, as compared to a response rate of 22% in patients with GCB DLBCL.


Lead Product(s): Mivavotinib

Therapeutic Area: Oncology Product Name: CB-659

Highest Development Status: Phase IIProduct Type: Small molecule

Partner/Sponsor/Collaborator: Not Applicable

Deal Size: Not Applicable Upfront Cash: Not Applicable

Deal Type: Not Applicable June 23, 2022

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The researchers then conducted multiple studies to validate the paralog gene pair, demonstrating that cells with VPS4B homozygous or heterozygous loss are sensitive to VPS4A knock down while cells without VPS4B loss are not.


Lead Product(s): Undisclosed

Therapeutic Area: Oncology Product Name: Undisclosed

Highest Development Status: PreclinicalProduct Type: Small molecule

Partner/Sponsor/Collaborator: Not Applicable

Deal Size: Not Applicable Upfront Cash: Not Applicable

Deal Type: Not Applicable April 08, 2022

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The preclinical data demonstrate that vacuolar protein sorting-associated protein 4A, VPS4A genetic inhibition in cell lines with loss of VPS4B preferentially showed profound death in cancer cells.


Lead Product(s): Undisclosed

Therapeutic Area: Oncology Product Name: Undisclosed

Highest Development Status: PreclinicalProduct Type: Small molecule

Partner/Sponsor/Collaborator: Not Applicable

Deal Size: Not Applicable Upfront Cash: Not Applicable

Deal Type: Not Applicable March 08, 2022

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Company will focus on advancing newly acquired targeted oncology compounds sapanisertib and mivavotinib, as well as the ongoing trial of CB-280 for the treatment of cystic fibrosis.


Lead Product(s): Telaglenastat,Pembrolizumab,Carboplatin

Therapeutic Area: Oncology Product Name: CB-839

Highest Development Status: Phase IIProduct Type: Small molecule

Partner/Sponsor/Collaborator: Not Applicable

Deal Size: Not Applicable Upfront Cash: Not Applicable

Deal Type: Not Applicable November 05, 2021

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CB-280 demonstrated linear pharmacokinetics with plasma exposure increasing proportionally with dose. CB-280 also demonstrated robust pharmacodynamic effects, with rapid and significant dose-proportional increases in plasma arginine, the key driver of NO production.


Lead Product(s): CB-280

Therapeutic Area: Genetic Disease Product Name: CB-280

Highest Development Status: Phase IProduct Type: Small molecule

Partner/Sponsor/Collaborator: Not Applicable

Deal Size: Not Applicable Upfront Cash: Not Applicable

Deal Type: Not Applicable November 01, 2021

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CB-280 is a potent and selective oral inhibitor of arginase significantly improved lung function and reduced Pseudomonas aeruginosa colony-forming units used in the treatment of Cystic Fibrosis.


Lead Product(s): CB-280

Therapeutic Area: Genetic Disease Product Name: CB-280

Highest Development Status: Phase IProduct Type: Small molecule

Partner/Sponsor/Collaborator: Not Applicable

Deal Size: Not Applicable Upfront Cash: Not Applicable

Deal Type: Not Applicable October 21, 2021

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Takeda to acquire two clinical-stage compounds, sapanisertib (CB-228, formerly TAK-228) and mivavotinib (CB-659, formerly TAK-659), both of which have demonstrated single-agent clinical activity with the greatest potential in biomarker-defined cancerpatient populations.


Lead Product(s): Sapanisertib

Therapeutic Area: Oncology Product Name: CB-228

Highest Development Status: PreclinicalProduct Type: Small molecule

Recipient: Takeda Pharmaceutical

Deal Size: $45.0 million Upfront Cash: $10.0 million

Deal Type: Acquisition October 18, 2021

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