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1d
Discovery of WWZ-11-098: a rigid and selective CDK6 degrader. (PubMed, Eur J Med Chem)
In addition, WWZ-11-098 displayed favorable pharmacokinetic properties (Cmax = 11833 ng/mL, T1/2 = 2.64 h after a 5 mpk IV dose) and exhibited robust antitumor efficacy (TGI: 77.1 % @10 mpk) in a MOLT-4 xenograft model without signs of toxicity. The compound provides not only a valuable chemical probe but also a lead structure for further development of CDK6 degraders.
Journal
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HER-2 (Human epidermal growth factor receptor 2) • CRBN (Cereblon) • CDK6 (Cyclin-dependent kinase 6) • CDK9 (Cyclin Dependent Kinase 9) • CDK1 (Cyclin-dependent kinase 1)
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HR positive • HER-2 negative
1d
Discover of a highly effective covalent inhibitor of CDK6 for triple-negative breast cancer treatment. (PubMed, Eur J Med Chem)
To overcome this challenge, we designed and synthesized a series of novel covalent inhibitors for CDK6 that contain the Palbociclib core pharmacophore...In vivo experiments further demonstrated that C32 has a favorable safety profile and pharmacokinetic properties, while exhibiting significant anti-TNBC effects. As a novel CDK6 covalent inhibitor, C32 is expected to be a candidate compound for the treatment of TNBC.
Journal
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HER-2 (Human epidermal growth factor receptor 2) • CDK6 (Cyclin-dependent kinase 6)
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HER-2 negative
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Ibrance (palbociclib)
3d
A Case of Suspected Contralateral Occult Breast Cancer Occurring a Decade Following Breast Cancer Surgery (PubMed, Gan To Kagaku Ryoho)
Postoperatively, the patient received TC(docetaxel+cyclophosphamide) chemotherapy, total breast irradiation, and tamoxifen for 10 years. Considering the different subtypes and absence of other lesions, the patient was considered to have latent breast cancer as a new lesion. Chemotherapy, including anti- HER2 therapy, radiotherapy, and endocrine therapy, was administered as adjuvant treatment.
Journal
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ER (Estrogen receptor) • GATA3 (GATA binding protein 3)
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HER-2 positive • ER positive • HER-2 negative • HER-2 negative + ER positive
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docetaxel • tamoxifen • cyclophosphamide
3d
A Case of Hormone Receptor-Positive, HER2-Negative Metastatic Recurrent Breast Cancer Successfully Treated with Capivasertib and Fulvestrant in Late-Line Therapy (PubMed, Gan To Kagaku Ryoho)
In the CAPItello-291 trial, capivasertib and fulvestrant demonstrated efficacy in patients with up to two prior lines endocrine therapy, but its use in late-line settings has not yet been reported. In this article, we report a case of a woman with metastatic recurrent breast cancer who was treated with capivasertib and fulvestrant was used as the late-line treatment, resulting in a progression-free survival of 8 months.
Journal
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HER-2 (Human epidermal growth factor receptor 2) • PIK3CA (Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha) • PTEN (Phosphatase and tensin homolog)
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HR positive • HER-2 negative • PIK3CA mutation • PTEN mutation • HR positive + HER-2 negative
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fulvestrant • Truqap (capivasertib)
3d
The Efficacy of CDK4/6 Inhibitors as Late Therapy in Patients Treated with Palbociclib and Abemaciclib Two Sequentially (PubMed, Gan To Kagaku Ryoho)
One PD and 6 adverse events were the reasons for switching to ABM after taking PLB. Although the number of patients was small, PFS with sequential CDK4/6 inhibitors could be expected to be longer than 6 months, suggesting that the treatment may be useful in extending the time to chemotherapy induction.
Retrospective data • Journal
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HER-2 (Human epidermal growth factor receptor 2)
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HER-2 positive • HR positive • HER-2 negative • HR positive + HER-2 negative
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Ibrance (palbociclib) • Verzenio (abemaciclib)
3d
A Case of Breast Cancer Initially Presenting with Opsoclonus-Myoclonus Syndrome (PubMed, Gan To Kagaku Ryoho)
Postoperatively, tamoxifen, a CDK4/6 inhibitor, and radiotherapy were administered...Despite initiating weekly paclitaxel plus bevacizumab, the disease progressed rapidly, and she died 4 months later. Notably, OMS symptoms did not recur. This case highlights paraneoplastic OMS as an initial manifestation of breast cancer, with neurological improvement following systemic therapy.
Journal
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HER-2 (Human epidermal growth factor receptor 2)
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HER-2 positive • HR positive • HER-2 negative • HR positive + HER-2 negative
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Avastin (bevacizumab) • paclitaxel • tamoxifen
3d
Experience of Performing Liver Biopsy in Combination with TAE for Recurrence of HR-Positive HER2-Negative Breast Cancer with Rapid Appearance of Organ Metastases (PubMed, Gan To Kagaku Ryoho)
After irradiation to the pain area, paclitaxel and bevacizumab therapy was administered, and a marked reduction of pulmonary and liver metastases, and the disappearance of pain were observed. Local hepatic therapy with TAE followed by chemotherapy was thought to have helped the patient overcome the rapid tumor growth.
Journal
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HER-2 (Human epidermal growth factor receptor 2)
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HER-2 positive • HR positive • HER-2 negative • HR positive + HER-2 negative
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Avastin (bevacizumab) • paclitaxel
3d
Pleomorphic Invasive Lobular Carcinoma Developed after Surgery for Simultaneous Ipsilateral Multiple Cancers (PubMed, Gan To Kagaku Ryoho)
The results were ER negative, PgR positive, HER2 negative, and Ki-67 25%. As the prognosis and treatment of invasive lobular carcinoma was unclear, caution was required.
Journal
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HER-2 (Human epidermal growth factor receptor 2) • ER (Estrogen receptor) • PGR (Progesterone receptor)
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HER-2 negative • ER negative • PGR positive
3d
A Case Study of Severe Myelosuppression Induced by Adjuvant Chemotherapy in a Breast Cancer Patient with Concurrent Immune Thrombocytopenia(ITP) (PubMed, Gan To Kagaku Ryoho)
Following completion of weekly paclitaxel(PTX), initiation of epirubicin plus cyclophosphamide(EC)resulted in a marked platelet decrease to 1.3×104/μL on day 7, necessitating repeated platelet transfusions. These findings suggest that in breast cancer patients with ITP, neoadjuvant chemotherapy may not be feasible, and primary surgical intervention should be considered. Furthermore, when administering EC, vigilant hematological monitoring is imperative.
Journal
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ER (Estrogen receptor)
|
HER-2 negative • ER negative
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paclitaxel • cyclophosphamide • epirubicin
3d
Two Cases of Node-Positive Breast Cancer in Which the Oncotype DX Test Was Performed but Yielded Inconclusive Results (PubMed, Gan To Kagaku Ryoho)
Three lymph node metastases were identified. Oncotype DX was performed but was judged inconclusive due to insufficient tumor tissue.
Journal
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HER-2 (Human epidermal growth factor receptor 2)
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HR positive • HER-2 negative • HR positive + HER-2 negative
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Oncotype DX Breast Recurrence Score®Test
3d
A Case of Early Breast Cancer Which Transient CEA Elevation after Treatment with Immune Checkpoint Inhibitors (PubMed, Gan To Kagaku Ryoho)
The efficacy of perioperative treatment with pembrolizumab for early-stage triple-negative breast cancer(TNBC)at high risk of recurrence was demonstrated in the KEYNOTE-522 trial, and it's indication was expanded in Japan as of September 2022...As follow-up continued, CEA levels began to decline and the thymic enlargement showed a tendency to regress. These findings suggest a potential association between immune checkpoint inhibitor and thymic enlargement, as well as a possible link to the observed CEA elevation.
Journal • Checkpoint inhibition
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HER-2 (Human epidermal growth factor receptor 2) • ER (Estrogen receptor) • PGR (Progesterone receptor)
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HER-2 negative • ER negative
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Keytruda (pembrolizumab)