Therapy Detail

Therapy Name Pictilisib
Therapy Description

Pictilisib (GDC-0941) inhibits isoforms of PI3K, which inhibits PI3K/AKT signaling resulting in antitumor activity, including inhibition of tumor growth (PMID: 19584227).

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Drug Name Trade Name Synonyms Drug Classes Drug Description
Pictilisib GDC-0941 PI3K Inhibitor (Pan) 34 Pictilisib (GDC-0941) inhibits isoforms of PI3K, which inhibits PI3K/AKT signaling resulting in antitumor activity, including inhibition of tumor growth (PMID: 19584227).
Molecular Profile Indication/Tumor Type Response Type Therapy Name Approval Status Evidence Type Efficacy Evidence References
KRAS mutant pancreatic cancer decreased response Pictilisib Preclinical - Cell line xenograft Actionable In a preclinical study, Pictilisib (GDC-0941) demonstrated limited efficacy as a single agent in pancreatic cell line xenograft models harboring KRAS mutations (PMID: 22952903). 22952903
KRAS G12D myelodysplastic/myeloproliferative neoplasm sensitive Pictilisib Preclinical Actionable In a preclinical study, Pictilisib (GDC-0941) demonstrated efficacy in a mouse model of chronic myelomonocytic leukemia expressing KRAS G12D (ASH Annual Meeting Abstracts 2012 120: 2862). detail...
KRAS G12D pancreatic cancer decreased response Pictilisib Preclinical - Cell line xenograft Actionable In a preclinical study, Pictilisib (GDC-0941) demonstrated limited efficacy as a single agent in a pancreatic cell line xenograft model harboring KRAS G12D (PMID: 22952903). 22952903
PTEN loss RB1 loss triple-receptor negative breast cancer resistant Pictilisib Preclinical Actionable In a preclinical study, a triple-receptor negative breast cancer line harboring PTEN and RB1 loss was resistant to Pictilisib (GDC-0941) induced growth inhibition in culture (PMID: 27020857). 27020857
BRAF mut PTEN inact mut melanoma sensitive Pictilisib Preclinical Actionable In a preclincal study, Pictilisib (GDC-0941) inhibited Akt activation and proliferation in melanoma cell lines harboring BRAF mutations and PTEN inactivating mutations in culture (PMID: 26577700). 26577700
PTEN inact mut estrogen-receptor positive breast cancer sensitive Pictilisib Preclinical - Cell culture Actionable In a preclinical study, a PTEN deficient estrogen-receptor (ER) positive breast cancer cell line demonstrated increased sensitivity to treatment in culture when Pictilisib (GDC-0941) was given at a higher dose for a shorter duration, resulting in inhibition of cell growth (PMID: 26733612). 26733612
PTEN N48I urinary bladder cancer decreased response Pictilisib Preclinical - Cell culture Actionable In a preclinical study, Pictilisib (GDC-0941) demonstrated limited inhibition of Akt phosphorylation and growth in bladder cancer cells harboring PTEN N48I in culture (PMID: 28808038). 28808038
PTEN loss STK11 loss endometrial cancer sensitive Pictilisib Preclinical Actionable In a preclinical study, the PI3K inhibitor GDC-0941 reduced tumor growth rate in immunodeficient mice engrafted with endometrial tumors from PTEN/STK11 (LKB1) deficient mice (PMID: 24322983). 24322983
KRAS Q61H non-small cell lung carcinoma resistant Pictilisib Preclinical Actionable In a preclinical study, a human non-small cell lung cancer cell line harboring KRAS Q61H (PMID: 19165201) were insensitive to pictilisib (GDC-0941) growth inhibition in culture (PMID: 22693356). 22693356 19165201
Unknown unknown islet cell tumor not applicable Pictilisib Preclinical Actionable In a preclinical study, Pictilisib (GDC-0941) inhibited AKT activation, reduced tumor burden, and increased lifespan in a transgenic mouse model of pancreatic neuroendocrine tumor (PMID: 27225693). 27225693
PTEN loss non-small cell lung carcinoma sensitive Pictilisib Preclinical - Cell line xenograft Actionable In preclinical studies, the PI3K inhibitor GDC-0941 demonstrated efficacy against NSCLC tumor cell lines in both culture and xenograft models harboring alterations in the PI3K pathway (PMID: 23136191). 23136191
Clinical Trial Phase Therapies Title Recruitment Status
NCT01493843 Phase II Carboplatin Pictilisib Bevacizumab Study Evaluating the Safety and Efficacy of Carboplatin/Paclitaxel and Carboplatin/Paclitaxel/Bevacizumab With and Without GDC-0941 in Patients With Previously Untreated Advanced or Recurrent Non-small Cell Lung Cancer Completed
NCT01437566 Phase II GDC-0980 Fulvestrant Pictilisib Study of GDC-0941 or GDC-0980 With Fulvestrant Versus Fulvestrant in Advanced or Metastatic Breast Cancer in Patients Resistant to Aromatase Inhibitor Therapy Completed