tucatinib

receptor tyrosine kinase inhibitor for tratment of HER2 positive breast cancer

Also Known As:

N6-(4,4-Dimethyl-4,5-dihydrooxazol-2-yl)-N4-(3-methyl-4-((1,2,4)triazolo(1,5-a)pyridin-7-yloxy)phenyl)quinazoline-4,6-diamine; N6-(4,5-dihydro-4,4-dmethyl-2-oxazolyl)-N4-(3-methyl-4-((1,2,4)triazolo(1,5-A)pyridin-7-Yloxy)phenyl)-4,6-quinazolinediamine; ONT-380; irbinitinib; tukysa

Networked: 93 relevant articles (23 outcomes, 21 trials/studies)

Relationship Network

Bio-Agent Context: Research Results

Heterocyclic Compounds: 198
- 1-Ring Heterocyclic Compounds
  - Azoles: 2138
    - Oxazoles: 89
      - tucatinib: 93
  - Pyridines: 88
    - tucatinib: 93
- Fused-Ring Heterocyclic Compounds
  - 2-Ring Heterocyclic Compounds
    - Quinazolines: 402
      - tucatinib: 93

Experts

1.	Borges, Virginia F: 5 articles (01/2022 - 07/2017)
2.	Hamilton, Erika: 5 articles (01/2021 - 01/2018)
3.	Gelmon, Karen: 4 articles (01/2022 - 01/2020)
4.	Alley, Stephen C: 3 articles (01/2022 - 01/2021)
5.	Ferrario, Cristiano: 3 articles (01/2022 - 01/2018)
6.	Lee, Anthony J: 3 articles (01/2022 - 01/2021)
7.	Vo, Alex: 3 articles (01/2022 - 01/2018)
8.	Krop, Ian: 3 articles (12/2021 - 01/2018)
9.	Cameron, David: 3 articles (01/2021 - 01/2020)
10.	Curigliano, Giuseppe: 3 articles (01/2021 - 01/2020)

Related Diseases

1.	Breast Neoplasms (Breast Cancer) 01/01/2022 - "The efficacy of tucatinib-based therapeutic approaches for HER2-positive breast cancer." 12/01/2021 - "Study participants will receive treatment with T-DM1 and placebo (a pill that looks like the study drug but contains no medication) or T-DM1 and tucatinib, for up to 14 cycles, unless their breast cancer returns or the side effects become too severe. " 02/12/2023 - "The Value of Tucatinib in Metastatic HER2-Positive Breast Cancer Patients: An Italian Cost-Effectiveness Analysis." 01/01/2023 - "This retrospective cohort study included patients diagnosed with HER2+ MBC (January 2017-December 2022) who received tucatinib treatment in a nationwide, de-identified electronic health record-derived metastatic breast cancer database. " 01/01/2023 - "We characterized the activity of tucatinib with the antibody–drug conjugate T-DM1 in preclinical models of breast cancer, including HER2-positive breast cancer cells and patient-derived xenograft (PDX) models. "
2.	Brain Neoplasms (Brain Tumor) 08/01/2023 - "All patients received tucatinib and SRS for the management of active brain metastases. " 01/01/2022 - "Combination of tucatinib and neural stem cells secreting anti-HER2 antibody prolongs survival of mice with metastatic brain cancer." 01/01/2021 - "Among patients with brain metastases (n = 164), risk of meaningful deterioration on EQ-VAS was reduced 49% in the tucatinib arm (HR: 0.51; 95% CI: 0.28, 0.93); the median (95% CI) time to deterioration was not reached in the tucatinib arm and was 5.5 months (4.2, -) in the placebo arm. " 01/01/2020 - "Among the patients with brain metastases, progression-free survival at 1 year was 24.9% in the tucatinib-combination group and 0% in the placebo-combination group (hazard ratio, 0.48; 95% CI, 0.34 to 0.69; P<0.001), and the median progression-free survival was 7.6 months and 5.4 months, respectively. " 01/01/2023 - "These results suggest that tucatinib may be the optimal TKI partner for HER2-targeted therapies and support clinical studies of its combination with T-DM1, including in patients with brain metastases. "
3.	Neoplasms (Cancer) 01/01/2022 - "This review highlights recent updates on the efficacy of tucatinib-based therapeutic approaches in experimental models as well as in the clinical settings of HER2+ breast cancer." 01/01/2023 - "We rationalized that combining tucatinib with other HER2-targeting agents with complementary mechanisms of action would further increase efficacy against tumors. " 01/01/2023 - "Tucatinib modulates the immune microenvironment favorably, and combination treatment with α-PD-L1 or α-PD-1 demonstrated increased efficacy in preclinical HER2-positive tumor models. " 07/15/2017 - "This Phase I study determined the MTD, pharmacokinetics (PK) and antitumor activity of ONT-380 in HER2-positive advanced solid tumors, with an expansion cohort of patients with HER2+ MBC.Experimental" 11/08/2023 - "1 out of 30 participants had their tumors respond to treatment with tucatinib alone within 12 weeks. "
4.	Colorectal Neoplasms (Colorectal Cancer) 05/01/2022 - "Tucatinib: an investigational novel therapeutic agent for the treatment of HER-2 colorectal cancer." 07/01/2020 - "Tucatinib is an oral, small molecule, selective HER2 inhibitor initially developed by Array BioPharma (a subsidiary of Pfizer) and subsequently developed by Seattle Genetics for the treatment of HER2-positive solid tumours, including breast cancer and colorectal cancer. " 11/08/2023 - "A study to learn how well tucatinib plus trastuzumab works for treating participants with metastatic colorectal cancer, and how safe it is: a plain language summary of the MOUNTAINEER study." 11/08/2023 - "Tucatinib with trastuzumab could be a good treatment option for people with HER2-positive colorectal cancer that has spread to other parts of the body. " 01/01/2023 - "Tucatinib plus trastuzumab for chemotherapy-refractory, HER2-positive, RAS wild-type unresectable or metastatic colorectal cancer (MOUNTAINEER): a multicentre, open-label, phase 2 study."
5.	Leukemia 01/01/2021 - "In the present study, the results demonstrated that tucatinib significantly improved the efficacy of conventional chemotherapeutic agents in ABCG2‑overexpressing leukemia cells and primary leukemia blast cells, derived from patients with leukemia. " 01/01/2021 - "In SP cells, isolated from leukemia cells, the intracellular accumulation of Hoechst 33342, which is an ABCG2 substrate, was significantly elevated by tucatinib. " 01/01/2021 - "In addition, tucatinib markedly decreased the proportion of leukemia stem cell‑like side population (SP) cells. " 01/01/2021 - "In vitro and ex vivo anti‑tumor effect and mechanism of Tucatinib in leukemia stem cells and ABCG2‑overexpressing leukemia cells." 01/01/2021 - "The present study revealed that combined treatment with tucatinib and conventional cytotoxic agents could be a potential therapeutic strategy in ABCG2‑positive leukemia."

Related Drugs and Biologics

1.	Trastuzumab (Herceptin)
2.	Capecitabine (Xeloda)
3.	human ERBB2 protein
4.	Tyrosine Kinase Inhibitors
5.	neratinib
6.	Lapatinib (GW572016)
7.	trastuzumab deruxtecan
8.	pertuzumab
9.	ErbB Receptors (EGF Receptor)
10.	palbociclib

Related Therapies and Procedures

1.	Therapeutics
2.	Drug Therapy (Chemotherapy)
3.	Ambulatory Care (Outpatient Care)
4.	Immunotherapy
5.	Aftercare (After-Treatment)