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Development Status

Investigational

3

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Primary Target

PI3-kinase class I

2

PI3-kinase p110-alpha subunit

1

PI3-kinase p110-beta subunit

1

PI3-kinase p110-delta subunit

1

PI3-kinase p110-gamma subunit

1

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Highest Phase

Phase II

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Approval Year

Unknown

3

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Condition

Breast cancer

3

Non-small cell lung cancer

2

Endometrial cancer

1

Prostate cancer

1

Renal cell carcinoma

1

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Treatment Modality

Primary

3

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CNS Activity

CNS Non-penetrant

3

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Originator

Piramed Pharma|Genentech|Institute of Cancer Research|Breakthrough Breast Cancer Research Centre

2

Genentech|Piramed

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Substance Class

Chemical

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Code System

CAS

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FDA UNII

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NCI_THESAURUS

3

PUBCHEM

3

ChEMBL

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Substance Form

Principal Form

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Salts, Hydrates, Esters, etc.

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Showing 1 - 3 of 3 results

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APITOLISIB

1C854K1MIJ

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Status:

Investigational

Class (Stereo):

CHEMICAL (ABSOLUTE)

Targets:

PI3-kinase p110-beta subunit

Serine/threonine-protein kinase mTOR

PI3-kinase p110-alpha subunit

PI3-kinase p110-delta subunit

PI3-kinase p110-gamma subunit

Conditions:

Renal cell carcinoma

Endometrial cancer

Prostate cancer

Apitolisib, a dual inhibitor of mTOR and phosphatidylinositol 3-kinase (PI3K), was being developed by Roche and Genentech as an orally administered therapy of cancer. Apitolisib is a selective, potent, orally bioavailable inhibitor of Class I PI3 kin...

ase (PI3K) and mTOR kinase (TORC1/2) with excellent pharmacokinetic and pharmaceutical properties. Apitolisib displayed excellent potency against class I PI3K isoforms (IC50 PI3K-α, β, δ and γ = 4.8, 27, 6.7 and 14 nM) and mTOR kinase (IC50 = 17 nM) and selectivity against a large panel of other kinases. Apitolisib is in phase II trials by Genentech for the treatment of breast cancer, prostate cancer, endometrium cancer, kidney cancer. However, no recent development has been reported. It is also in phase I trials by Genentech for the treatment of non-Hodgkin's lymphoma.

PICTILISIB

ICY00EMP8P

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Status:

Investigational

Class (Stereo):

CHEMICAL (ACHIRAL)

Targets:

PI3-kinase class I

Conditions:

Non-small cell lung cancer

Pictilisib is an oral potent inhibitor of class I PI3K with nanomolar activities against p110alpha, p110beta, p110delta, and p110gamma. The drug was developed for the treatment of solid tumors and reached phase II in patients with breast cancer and ...

lung carcinoma, however its development was terminated.

PICTILISIB BISMESYLATE

G3D7HF2GS9

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Status:

Investigational

Class (Stereo):

CHEMICAL (ACHIRAL)

Targets:

PI3-kinase class I

Conditions:

Non-small cell lung cancer

Pictilisib is an oral potent inhibitor of class I PI3K with nanomolar activities against p110alpha, p110beta, p110delta, and p110gamma. The drug was developed for the treatment of solid tumors and reached phase II in patients with breast cancer and ...

lung carcinoma, however its development was terminated.

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