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Restrict the search for
tyrosine
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Status:
Investigational
Source:
INN:evobrutinib [INN]
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Evobrutinib is a highly selective, irreversible inhibitor of Bruton's tyrosine kinase (BTK). It potently inhibits BCR- and Fc receptor-mediated signaling and, thus, subsequent activation and function of B cells and innate immune cells such as monocytes and basophils. Evobrutinib demonstrated effectivity in autoimmune disease preclinical models. Evobrutinib is being developed by Merck Serono for the treatment of various autoimmune disorders.
Status:
Investigational
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Conditions:
Tozasertib, originally developed as VX-680 by Vertex (Cambridge, MA) and later renamed MK-0457 by Merck (Whitehouse Station, NY), was the first aurora kinase inhibitor to be tested in clinical trials. The drug, a pyrimidine derivative, has affinity for all aurora family members at nanomolar concentrations with inhibitory constant values (Ki(app)) of 0.6, 18, and 4.6 nM for aurora A, aurora B, and aurora C, respectively. Preclinical studies confirmed that tozasertib inhibited both aurora A and aurora B kinase activity, and activity has been reported against prostate, thyroid, ovarian, and oral squamous cancer cell lines. Upon treatment with tozasertib, cells accumulate with a 4N DNA content due to a failure of cytokinesis. This ultimately leads to apoptosis, preferentially in cells with a compromised p53 function. Tozasertib is an anticancer chemotherapeutic pan-aurora kinase (AurK) inhibitor that also inhibits FMS-like tyrosine kinase 3 (FLT3) and Abl. Tozasertib is currently in clinical trials as a potential treatment for acute lymphoblastic leukemia (ALL). In cellular models of cancer, tozasertib activates caspase-3 and PARP and decreases expression of HDAC, increasing apoptosis and inhibiting cell growth. In other cellular models, tozasertib inhibits cell proliferation and metastasis by blocking downstream ERK signaling and downregulating cdc25c and cyclin B. This compound also decreases tumor growth in an in vivo model of prostate cancer.
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Canertinib or CI-1033 (N-[4-[N-(3-Chloro-4-fluorophenyl)amino]-7-[3-(4-morpholinyl)propoxy]quinazolin-6-yl]acrylamide) is a pan-erbB tyrosine kinase inhibitor. It selectively inhibits erbB1 (epidermal growth factor receptor), erbB2, erbB3, and erbB4 without inhibiting tyrosine kinase activity of receptors such as platelet-derived growth factor receptor, fibroblast growth factor receptor, and insulin receptor, even at high concentrations. Canertinib was under development by Pfizer Inc as a potential treatment for cancer.
Status:
Investigational
Class (Stereo):
CHEMICAL (ACHIRAL)
Sivifene (also known as A-007), a triaryl hydrazone that produced objective responses when applied topically. During preclinical studies, sivifene was observed to upregulate both cutaneous and systemic T-lymphocytes, in particular, CD4/8+ lymphocyte subtypes. The current mechanism of action for the drug is unknown however is assumed that it can show its immunomodulating properties through the upregulation of the CD45 T lymphocyte cell surface receptor. Sivifene was being evaluated for its anticancer activities in melanoma, breast cancer, Kaposi's sarcoma, and lymphoproliferative disorders. The drug as a 0.25% gel is confirmed as an effective palliative treatment option for cutaneous metastases from cancers. Skin reactions were minimal, tolerated, and no cessation of treatment was required. However, the further development of this drug apparently has been discontinued.
Status:
Investigational
Class (Stereo):
CHEMICAL (ACHIRAL)
Linsitinib is an inhibitor of the insulin receptor and the insulin-like growth factor 1 receptor, which may result in the inhibition of tumor cell proliferation and the induction of tumor cell apoptosis. Linsitinib is in phase II clinical trials for the treatment of metastatic prostate carcinoma, gastrointestinal stromal tumors and other cancers. Common adverse events included fatigue, nausea hyperglycaemia and anorexia.
Status:
Investigational
Source:
INN:rocbrutinib [INN]
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Status:
Investigational
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Foretinib is an orally available multikinase inhibitor that targets c-MET and VEGFR2 with high affinity, which may result in the inhibition of tumor angiogenesis, tumor cell proliferation and metastasis. Foretinib is an experimental drug candidate for the treatment of cancer. It was in Phase II trials for the treatment breast cancer, non-small cell lung cancer, gastric cancer, head and neck cancer and papillary renal-cell carcinoma. The most frequent adverse events of any grade associated with foretinib were fatigue, hypertension, gastrointestinal toxicities, and nonfatal pulmonary emboli.
Status:
Investigational
Source:
INN:detrothyronine [INN]
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Detrothyronine is the (R)-(D)-form of triiodothyronine and has antihyperlipidaemic actions with beneficial effects upon coronary disease and hypertension. Detrothyronine has been tried in the treatment of hypercholesterolemia but its toxic effects outweigh any therapeutic advantage.
Status:
Investigational
Source:
INN:ertiprotafib [INN]
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Ertiprotafib was originally developed as an inhibitor of PTP1B. Multiple targets of ertiprotafib, in addition to PTP1B inhibition, have been suggested including dual PPARalpha/PPARgamma agonism and IKK-beta inhibition. It normalized the plasma glucose and insulin levels in diabetic animal models and progressed to a phase II clinical trial for the treatment of Type 2 diabetes mellitus. Ertiprotafib development has been discontinued.
Status:
Investigational
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
