A bump and hole approach to the development of selective degrons by Brennan, PJ

“…Traditional IMiDs, such as thalidomide, lenalidomide and pomalidomide, are unsuitable for target validation due to off-target degradation of transcription factors IKZF1 and IKZF3, as well as other endogenous proteins.…”

The 5q- syndrome. by Giagounidis, A, Germing, U, Wainscoat, J, Boultwood, J, Aul, C

“…The most promising therapeutic approach is the novel thalidomide analogue CC5013 that is currently evaluated in an international phase II study.…”

Development and Validation of Pomalidomide Determination in Human Plasma by HPLC-MS/MS Method by T. N. Komarov, I. E. Shohin, M. A. Tokareva, O. A. Archakova, D. S. Bogdanova, A. A. Aleshina, N. S. Bagaeva, V. V. Davydanova, N. P. Sadchikova

“…Pomalidomide is used in case of previous multiple myeloma ineffective treatment. Pomalidomide is a thalidomide synthetic derived, approved as immunomodulatory drug by the Food and Drug Administration (FDA). …”
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Extrapolating empirical long-term survival data: the impact of updated follow-up data and parametric extrapolation methods on survival estimates in multiple myeloma by LJ Bakker, FW Thielen, WK Redekop, CA Uyl-de Groot, HM Blommestein

“…Methods Empirical data were available from a randomized controlled trial and a registry for MM patients treated with melphalan + prednisone, thalidomide, and bortezomib- based regimens. Standard parametric and spline models were fitted while artificially reducing follow-up by introducing database locks. …”
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Potential Drug Candidates in Clinical Trials for the Treatment of Covid-19: An Updated Overview by Osmar Ignacio Ayala Cáceres, Fernanda Timóteo, Kristiane Fanti Del Pino Santos, Rafael Rodrigo Piva Vasconcelos, Marco Antonio Utrera Martines, Juliana Jorge, Haroon ur Rashid

“…The pharmaceutical interventions evaluated for the treatment of Covid-19 include human immunoglobulin, interferons, chloroquine, hydroxychloroquine, arbidol, remdesivir, oseltamivir, favipiravir, carrimycin, methylprednisolone, bevacizumab, thalidomide, vitamin C, pyrodfenidone, darthviravir, bromexistone, ryrexavir, lopinavir, xiyanping, and traditional Chinese medicine. …”
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Sorafenib for the Treatment of Unresectable Hepatocellular Carcinoma: Preliminary Toxicity and Activity Data in Dogs by Laura Marconato, Silvia Sabattini, Giorgia Marisi, Federica Rossi, Vito Ferdinando Leone, Andrea Casadei-Gardini

“…The aim of this prospective, non-randomized, non-blinded, single center clinical trial was to investigate safety profile, objective response rate, time to progression and overall survival of sorafenib in comparison with metronomic chemotherapy (MC) consisting of thalidomide, piroxicam and cyclophosphamide in dogs with advanced, unresectable HCC. …”
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The influence of leprosy-related clinical and epidemiological variables in the occurrence and severity of COVID-19: A prospective real-world cohort study. by Selma Regina Penha Silva Cerqueira, Patrícia Duarte Deps, Débora Vilela Cunha, Natanael Victor Furtunato Bezerra, Daniel Holanda Barroso, Ana Bárbara Sapienza Pinheiro, Gecilmara Salviato Pillegi, Taynah Alves Rocha Repsold, Patrícia Shu Kurizky, Simon M Collin, Ciro Martins Gomes

“…Our model showed that the use of corticosteroids, thalidomide, pentoxifylline, clofazimine, or dapsone or BCG vaccination did not affect the occurrence or severity of COVID-19.…”
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Description of multiple myeloma cases and assessment of survival and mortality factors in Madagascar by Rova Malala Fandresena Randrianarisoa, Valéry Refeno, Ny Ony Tiana Florence Andrianandrasana, Fidiarivony Ralison, Hanta Marie Danielle Vololontiana, Florine Rafaramino

“…The combination of melphalan-prednisone-thalidomide was used in 79.63% of cases, and one patient had received autologous stem cell transplantation. …”
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Supportive Care in Cancer Cachexia: Meeting the Unmet Need by Abhishek Shankar, Pritanjali Singh, Seema Mishra, Shipra Gupta, Shubham Roy, Deepak Saini, Sachidanand Jee Bharati, Tulika Seth, Apoorva Maheshwari, Ajeet Kumar

“…Pharmacological interventions for neoplastic cachexia include drugs that stimulate the appetite: megestrol acetate (MA) and dronabinol; cytokine inhibitors (such as cyproheptadine, thalidomide, pentoxifylline and an eicosapentaenoic acid (EPA)); and anabolic agents such as nandrolone decanoate, oxandrolone and corticosteroids. …”
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Multiple-Drugs-Related Osteonecrosis of the Jaw in a Patient Affected by Multiple Myeloma: A Case Report by Mario Caggiano, Federica Di Spirito, Alfonso Acerra, Marzio Galdi, Laura Sisalli

“…A 60-year-old woman suffering from multiple myeloma (MM) was treated with zoledronic acid (bisphosphonate), dexamethasone (corticosteroid), bortezomib (a chemotherapeutic agent), and lenalidomide (thalidomide analog) for about a year and with lenalidomide alone as maintenance therapy for almost two years and developed stage three medication-related osteonecrosis of the jaws (MRONJ) in the upper left dental arch approximately two weeks after tooth extraction, which was treated with a medical nonoperative conservative approach until reversion to stage one. …”
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Autologous Stem Cell Transplantation in Multiple Myeloma: Where Are We and Where Do We Want to Go? by Sonia Morè, Laura Corvatta, Valentina Maria Manieri, Francesco Saraceni, Ilaria Scortechini, Giorgia Mancini, Alessandro Fiorentini, Attilio Olivieri, Massimo Offidani

“…The introduction of high-dose therapy in the 1990s as well as the development of drugs such as thalidomide, lenalidomide, and bortezomib in the 2000s led to an impressive improvement in outcome of patients with multiple myeloma (MM) eligible for autologous stem cell transplantation (ASCT). …”
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Synthesis and Preliminary Characterization of Putative Anle138b-Centered PROTACs against α-Synuclein Aggregation by Martina Pedrini, Angelo Iannielli, Lorenzo Meneghelli, Daniele Passarella, Vania Broccoli, Pierfausto Seneci

“…The search for disease-modifying agents targeted against Parkinson’s disease led us to rationally design a small array of six Anle138b-centered PROTACs, <b>7a</b>,<b>b</b>, <b>8a</b>,<b>b</b> and <b>9a</b>,<b>b</b>, targeting αSynuclein (αSyn) aggregates for binding, polyubiquitination by the E3 ligase Cereblon (CRBN), and proteasomal degradation. Lenalidomide and thalidomide were used as CRBN ligands and coupled with amino- and azido Anle138b derivatives through flexible linkers and coupling reactions (amidation, ‘click’ chemistry). …”
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Synthesis, Characterization, and Biological Evaluation of Gabapentinoid Hybrids with Isoindole-1,3(2H)-Dione Moiety as Potential Antioxidant, Antimicrobial, and Anticancer Agents by Mirna Jabbour, Mohammad Ammar Al-Khayat, Mahmoud Al-Ktaifani

“…Compound 2 is highly effective against Caco-2 cells and more effective than thalidomide, with IC50 value less than 1 μmol/L. Conclusion. …”
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Tumor necrosis factor inhibitors and janus kinase inhibitors in the treatment of cicatricial alopecia: A systematic review. by Nima Hajizadeh, Amirhossein Heidari, Sara Sadeghi, Azadeh Goodarzi

“…As a TNF inhibitor, adalimumab induced a rapid and stable improvement in signs and symptoms in most patients with rare, tolerable AEs. Thalidomide was the other frequently reported yet controversial TNF inhibitor, which caused a rapid and significant improvement in the condition. …”
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Three-year progression-free survival of a patient with concomitant mucinous adenocarcinoma of the colon with peritoneal dissemination and multiple myeloma who received lenalidomide... by Koki Tamai, Hajime Hirose, Yo Akazawa, Yukihiro Yoshikawa, Masatoshi Nomura, Hiroshi Takeyama, Masahiro Tokunaga, Mitsuyoshi Tei, Shu Okamura, Yusuke Akamaru

“…Lenalidomide is an oral thalidomide analog drug used for MM. Recently, the antitumor effect of lenalidomide has been gaining attention, and lenalidomide has been applied for managing solid tumors. …”
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Mechanisms of Immune Evasion in Multiple Myeloma: Open Questions and Therapeutic Opportunities by Cirino Botta, Francesco Mendicino, Enrica Antonia Martino, Ernesto Vigna, Domenica Ronchetti, Pierpaolo Correale, Fortunato Morabito, Antonino Neri, Massimo Gentile

“…Indeed, it is not a case that the most important drugs for the treatment of MM include immunomodulatory agents (thalidomide, lenalidomide, and pomalidomide) and monoclonal antibodies (daratumumab, isatuximab, and elotuzumab). …”
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Lenalidomide attenuates IMQ-induced inflammation in a mouse model of psoriasis by Hai-Yan Jia, Hai-Ying Qiu, Meng-Di Zhang, Jing-Jing Hou, Meng-Lu Zhou, Yan Wu

“…Lenalidomide (Len) is a structural analog of thalidomide, which belongs to the second generation of immunomodulators and has the functions of tumor killing, immune regulation, anti-angiogenesis and regulation of the myeloma microenvironment. …”
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Combined Use of Ninjin'yoeito Improves Subjective Fatigue Caused by Lenalidomide in Patients With Multiple Myeloma: A Retrospective Study by Tomoki Ito, Akiko Konishi, Yukie Tsubokura, Yoshiko Azuma, Masaaki Hotta, Hideaki Yoshimura, Takahisa Nakanishi, Shinya Fujita, Aya Nakaya, Atsushi Satake, Kazuyoshi Ishii, Shosaku Nomura

“…Lenalidomide is an immunomodulating derivative of thalidomide, which shows anti-tumor activity against myeloma cells with immunomodulation including augmentation of T-cell and natural killer cell function. …”
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ERBB1/EGFR and JAK3 Tyrosine Kinases as Potential Therapeutic Targets in High-Risk Multiple Myeloma by Fatih M. Uckun, Sanjive Qazi

“…We first compared the transcriptomes of malignant plasma cells from newly diagnosed MM patients who were risk-categorized based on the patient-specific EMC-92/SKY-92 gene expression signature values vs. normal plasma cells from healthy volunteers using archived datasets from the HOVON65/GMMG-HD4 randomized Phase 3 study evaluating the clinical efficacy of bortezomib induction/maintenance versus classic cytotoxic drugs and thalidomide maintenance. In particular, ERBB1/EGFR was significantly overexpressed in MM cells in comparison to normal control plasma cells, and it was differentially overexpressed in MM cells from high-risk patients. …”
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Use of Minimal Residual Disease Status to Reduce Uncertainty in Estimating Long-term Survival Outcomes for Newly Diagnosed Multiple Myeloma Patients by Naomi van Hest, Peter Morten, Keith Stubbs, Nicola Trevor

“…**Methods:** Standard and response-based PSMs, estimating patient life-years (LYs) over a lifetime horizon, were developed for NDMM patients treated with bortezomib, thalidomide, and dexamethasone (BTd) with or without daratumumab as induction and consolidation therapy. …”
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