Drugs / Ipatasertib
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Ipatasertib

also known as GDC-0068 · ipat · RG-7440

Small molecule targets AKT1 via inhibition

Developed for
breast cancer · cancer · triple-negative breast carcinoma · cancer of unknown primary site · estrogen-receptor positive breast cancer · female breast carcinoma · non-small cell lung carcinoma · breast neoplasm
+25 more · castration-resistant prostate carcinoma · glioblastoma · hypopharynx squamous cell carcinoma · laryngeal squamous cell carcinoma · metastatic malignant neoplasm · metastatic prostate carcinoma · neoplasm · oropharynx squamous cell carcinoma · ovarian cancer · plasma cell myeloma · prostate cancer · adult lymphoma · digestive system cancer · endometrial cancer · endometrial endometrioid adenocarcinoma · gastric adenocarcinoma · gastric cancer · high grade malignant neoplasm · maxillary sinus squamous cell carcinoma · nasal cavity squamous cell carcinoma · oral cavity squamous cell carcinoma · ovarian endometrioid adenocarcinoma · ovarian serous adenocarcinoma · refractory malignant neoplasm · solid adenocarcinoma with mucin production
Investigated by
Hoffmann-La Roche · Genentech, Inc. · National Cancer Institute (NCI) · MedSIR · Pfizer · Canadian Cancer Trials Group
+31 more · Foundation Medicine · German Cancer Research Center · NRG Oncology · Queen Mary University of London · SOLTI Breast Cancer Research Group · Aarhus University Hospital · Alliance Foundation Trials, LLC. · Asan Medical Center · BC Cancer Foundation · Canadian Cancer Clinical Trials Network · City of Hope Medical Center · David VanderWeele · ECCO - the European CanCer Organisation · Eli Lilly and Company · European Network of Gynaecological Oncological Trial Groups (ENGOT) · Fondazione per la Medicina Personalizzata · GOG Foundation · Gilead Sciences · Hospices Civils de Lyon · Institute of Cancer Research, United Kingdom · Jun Zhang, MD, PhD · Kliniken Essen-Mitte · Massachusetts General Hospital · Medical Research Council · Merck Sharp & Dohme LLC · NCRI Clinical Studies Groups · Roche Pharma AG · Royal Marsden NHS Foundation Trust · University of Iowa · University of Kentucky · Westdeutsche Studiengruppe GmbH (WSG)

Trials 54 · a red edge is where a trial was stopped

PhaseRegistry idDatesIndicationSponsorStatusOutcome
Phase 117 trials
Phase 1 NCT05172245 Sep 2022 → Jul 2027 expected cancer of unknown primary site, hypopharynx squamous cell carcinoma, laryngeal squamous cell carcinoma, maxillary sinus squamous cell carcinoma +2 National Cancer Institute (NCI) Recruiting No outcome recorded
Phase 1 NCT05276973 Sep 2022 → Jan 2025 overdue fallopian tube endometrioid adenocarcinoma, fallopian tube serous adenocarcinoma, ovarian endometrioid adenocarcinoma, ovarian serous adenocarcinoma +1 National Cancer Institute (NCI) Active not recruiting No outcome recorded
Phase 1 NCT04341259 Nov 2020 → Apr 2023 cancer Hoffmann-La Roche Completed No outcome recorded
Phase 1 NCT04404140 Jul 2020 → Oct 2022 castration-resistant prostate carcinoma Hoffmann-La Roche Terminated No outcome recorded
Phase 1 NCT04253561 Feb 2020 → Dec 2021 breast cancer SOLTI Breast Cancer Research Group Completed No outcome recorded
Phase 1 NCT04060862 Nov 2019 → Aug 2023 breast cancer Hoffmann-La Roche Terminated No outcome recorded
Phase 1 NCT03840200 Jun 2019 → Dec 2021 breast cancer, ovarian cancer, prostate cancer Hoffmann-La Roche Completed No outcome recorded
Phase 1 NCT03959891 May 2019 → Dec 2022 overdue breast cancer Massachusetts General Hospital Active not recruiting No outcome recorded
Phase 1 NCT03800836 Feb 2018 → Mar 2022 breast cancer Hoffmann-La Roche Completed No outcome recorded
Phase 1 NCT03341884 Nov 2017 → Jun 2018 liver disorder Genentech, Inc. Completed No outcome recorded
Phase 1/210 trials
Phase 1/2 NCT05538897 Mar 2023 → Jan 2027 expected endometrial endometrioid adenocarcinoma National Cancer Institute (NCI) Active not recruiting No outcome recorded
Phase 1/2 NCT04486352 Oct 2021 → Oct 2026 expected endometrial cancer Alliance Foundation Trials, LLC. Recruiting No outcome recorded
Phase 1/2 NCT04737109 Jul 2021 → Aug 2022 castration-resistant prostate carcinoma David VanderWeele Terminated No outcome recorded
Phase 1/2 NCT04802759 Jun 2021 → May 2029 expected estrogen-receptor positive breast cancer Hoffmann-La Roche Recruiting No outcome recorded
Phase 1/2 NCT03853707 Mar 2019 → Jan 2023 female breast carcinoma, triple-negative breast carcinoma City of Hope Medical Center Completed No outcome recorded
Phase 1/2 NCT03673787 Aug 2018 → Mar 2026 overdue glioblastoma, metastatic prostate carcinoma Institute of Cancer Research, United Kingdom Active not recruiting No outcome recorded
Phase 1/2 NCT03424005 Mar 2018 → Sep 2030 expected breast cancer Hoffmann-La Roche Recruiting No outcome recorded
Phase 1/2 NCT03337698 Dec 2017 → Oct 2025 non-small cell lung carcinoma Hoffmann-La Roche Terminated No outcome recorded
Phase 1/2 NCT03280563 Dec 2017 → Sep 2024 breast neoplasm Hoffmann-La Roche Completed No outcome recorded
Phase 1/2 NCT02430363 Mar 2013 → Jan 2016 glioblastoma Medical Research Council Unknown No outcome recorded
Phase 222 trials
Phase 2 NCT05554380 Sep 2023 → Aug 2026 high grade malignant neoplasm, metastatic malignant neoplasm National Cancer Institute (NCI) Suspended No outcome recorded
Phase 2 NCT05332561 Jun 2023 → Mar 2030 expected female breast carcinoma German Cancer Research Center Recruiting No outcome recorded
Phase 2 NCT05564377 Apr 2023 → Jul 2030 expected Her2-receptor negative breast cancer, endometrial carcinoma, fallopian tube carcinoma, female breast carcinoma +3 National Cancer Institute (NCI) Recruiting No outcome recorded
Phase 2 NCT04920708 Dec 2022 → Jun 2027 expected estrogen-receptor positive breast cancer Royal Marsden NHS Foundation Trust Active not recruiting No outcome recorded
Phase 2 NCT05172258 Jul 2022 → Jun 2027 expected hypopharynx squamous cell carcinoma, laryngeal squamous cell carcinoma, oral cavity squamous cell carcinoma, oropharynx squamous cell carcinoma National Cancer Institute (NCI) Active not recruiting No outcome recorded
Phase 2 NCT04551521 Oct 2021 → Dec 2024 cancer German Cancer Research Center Completed No outcome recorded
Phase 2 NCT04931342 Oct 2021 → Feb 2028 expected ovarian cancer Hoffmann-La Roche Active not recruiting No outcome recorded
Phase 2 NCT04467801 Sep 2021 → Aug 2024 non-small cell lung carcinoma Jun Zhang, MD, PhD Unknown No outcome recorded
Phase 2 NCT04739202 Mar 2021 → Jun 2026 gastric adenocarcinoma Hospices Civils de Lyon Completed No outcome recorded
Phase 2 NCT04589845 Jan 2021 → Sep 2032 expected cancer Hoffmann-La Roche Active not recruiting No outcome recorded
Phase 35 trials
Phase 3 NCT05862285 Jun 2023 → Mar 2033 expected cancer Hoffmann-La Roche Recruiting No outcome recorded
Phase 3 NCT04650581 Jan 2021 → May 2025 overdue breast cancer Canadian Cancer Trials Group Active not recruiting No outcome recorded
Phase 3 NCT04177108 Nov 2019 → Feb 2023 triple-negative breast carcinoma Hoffmann-La Roche Completed No outcome recorded
Phase 3 NCT03337724 Jan 2018 → Jan 2023 breast cancer Hoffmann-La Roche Completed No outcome recorded
Phase 3 NCT03072238 Jun 2017 → Mar 2020 metastatic prostate carcinoma Hoffmann-La Roche Completed No outcome recorded
Also used as a comparator or background therapy in 1 trial
PhaseRegistry idDatesIndicationSponsorStatusOutcome
Phase 2 NCT04561817 Comparator Oct 2020 → Oct 2022 ovarian cancer Icahn School of Medicine at Mount Sinai Withdrawn No outcome recorded

Press releases naming this drug 1 release

DateIssuerRelease
2020-06-19 Roche Global Development Roche’s IPATential150 study evaluating ipatasertib in combination with abiraterone and prednisone/prednisolone met one of its co-primary endpoints roche.com

Evidence & citations 8 cited values

Every value below carries the sentence it was read from. 57 sources stand behind the page.

FieldValueCited text
Known as ipatasertib Ipatasertib (GDC-0068) is a novel selective ATP-competitive small-molecule inhibitor of AKT that preferentially targets active phosphorylated AKT (pAKT)” PMID 27872130 Nov 2016
54

“200 mg oral ipatasertib followed 1 hour later by 80-mcg/800-nCi intravenous \[14C\]-ipatasertib on Day 1 of study” NCT02390492

Ipatasertib (GDC-0068) is a highly selective pan-Akt inhibitor targeting Akt1/2/3 .” NCT02430363

NCT04341259

NCT02162719

NCT04177108

NCT06400251

NCT05332561

NCT04589845

NCT04486352

NCT03280563

NCT04737109

NCT05276973

NCT03800836

NCT03498521

NCT01362374

NCT04591431

NCT04561817

NCT02301988

NCT03840200

NCT04650581

NCT04253561

NCT04920708

NCT05554380

NCT04739202

NCT03222310

NCT03673787

NCT03959891

NCT03337724

NCT03337698

NCT04464174

NCT02465060

NCT03853707

NCT04467801

NCT05172258

NCT02536391

NCT05172245

NCT05498896

NCT03424005

NCT03395899

NCT05538897

NCT05862285

NCT01896531

NCT04632992

NCT04060862

NCT04404140

NCT03385655

NCT03341884

NCT04551521

NCT03072238

NCT01562275

NCT05564377

NCT04802759

NCT02063581

NCT04931342

Known as GDC-0068 “A Phase I Study to Investigate the Absorption, Metabolism, and Excretion of \[14C\]-Ipatasertib (GDC-0068) Following a Single Oral Dose and to Investigate the Absolute...” NCT02390492
5

“A Phase Ib, Open-label, Dose-escalation Study of the Safety and Pharmacology of Ipatasertib (GDC-0068) in Combination With Docetaxel, Fluoropyrimidine Plus Oxaliplatin,...” NCT01362374

“A Study of Ipatasertib (GDC-0068) in Combination With Fluoropyrimidine Plus Oxaliplatin in Participants With Advanced or Metastatic Gastric or Gastroesophageal Junction Cancer” NCT01896531

“A Phase 1, Single-Dose, Randomized, Cross-Over, Relative Bioavailability, and Food Effect Study of Ipatasertib (GDC-0068) in Healthy Subjects” NCT02536391

“A Phase 1, Open-Label Study to Evaluate the Effect of Formulation on the Bioavailability of Ipatasertib (GDC-0068) in Healthy Subjects” NCT02063581

NCT01090960

Known as ipat ipatasertib (ipat) in combination with atezolizumab (atezo) and paclitaxel (pac) or nab-paclitaxel” NCT03800836
Known as RG-7440 ChEMBL registry synonym — accepted as the source's own label CHEMBL2177390
Action Inhibit “small-molecule inhibitor of AKT” PMID 27872130 Nov 2016
Modality Small molecule “Ipatasertib (GDC-0068) is a novel selective ATP-competitive small-molecule inhibitor of AKT” PMID 27872130 Nov 2016
Route Oral Oral repeating dose” NCT01090960
Target AKT1 “Ipatasertib (GDC-0068) is a highly selective pan-Akt inhibitor targeting Akt1/2/3 .” NCT02430363