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DRUG CLASS:

Microtubule inhibitor

Related drugs:
1d
Impact of genomic alterations measured in circulating tumor DNA (ctDNA) on clinical response to telisotuzumab vedotin treatment in patients with non-small cell lung cancer (NSCLC) (AIOM 2024)
METamp occurred more frequently in responders; but Teliso-V activity wasn’t restricted to these pts: most responders weren’t METamplified. Specific genomic alts beyond MET may influence clinical response. The current analysis demonstrated numeric differences between pts with identified drivers who did or didn’t respond to Teliso-V.
Clinical • Circulating tumor DNA
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EGFR (Epidermal growth factor receptor) • KRAS (KRAS proto-oncogene GTPase) • MET (MET proto-oncogene, receptor tyrosine kinase)
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KRAS G12C • MET amplification • KRAS G12
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Labcorp® Plasma Complete™
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telisotuzumab vedotin (ABBV-399)
1d
Mebendazole effectively overcomes imatinib resistance by dual-targeting BCR/ABL oncoprotein and β-tubulin in chronic myeloid leukemia cells. (PubMed, Korean J Physiol Pharmacol)
Meanwhile, MBZ directly targeted the colchicine-binding site of β-tubulin protein, hampered microtubule polymerization and induced mitosis arrest and mitotic catastrophe. This work discovered that anthelmintic MBZ exerts remarkable anticancer effects in both imatinib-sensitive and imatinib-resistant CML cells in vitro and revealed mechanisms underlying. From the perspective of drug repositioning and multi-target therapeutic strategy, this study provides a promising option for CML treatment, especially in TKI-resistant or intolerant individuals.
Journal
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ABL1 (ABL proto-oncogene 1)
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imatinib • mebendazole
1d
Anaplastic Large B-Cell Lymphoma: Cutaneous Presentations. (PubMed, Cureus)
This case underscores the importance of early biopsy and molecular testing when standard treatments fail. Early recognition and routine examinations, including lymph node assessments and skin biopsies, are critical for improving patient outcomes, as timely diagnosis leads to more effective treatment options and potential remission.
Journal
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ALK (Anaplastic lymphoma kinase) • TNFRSF8 (TNF Receptor Superfamily Member 8)
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TNFRSF8 expression • ALK negative
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Adcetris (brentuximab vedotin)
2d
FGFR Inhibitors in Urothelial Cancer: From Scientific Rationale to Clinical Development. (PubMed, J Korean Med Sci)
Among these therapies, erdafitinib, a pan-fibroblast growth factor receptor (FGFR) inhibitor for specific FGFR2 and FGFR3 alterations, is the only targeted therapy approved till now...Ongoing investigations exist on its use in non-muscle-invasive BC and in combination with drugs such as enfortumab vedotin in mUC...This review emphasizes the importance of FGFR inhibition in UC and the optimization of its use in clinical practice. Moreover, it underscores the ongoing efforts to evaluate combination strategies and early treatment testing to enhance the effectiveness of targeted therapies for UC.
Review • Journal • IO biomarker
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TP53 (Tumor protein P53) • FGFR2 (Fibroblast growth factor receptor 2) • FGFR3 (Fibroblast growth factor receptor 3) • RB1 (RB Transcriptional Corepressor 1)
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TP53 mutation • FGFR2 mutation • FGFR3 mutation
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Balversa (erdafitinib) • Padcev (enfortumab vedotin-ejfv)
3d
Utidelone combined with anti‑angiogenic therapy for the treatment of anthracycline/taxane‑treated and endocrine‑resistant HR+/HER2‑ refractory breast cancer with brain metastases: A case report. (PubMed, Oncol Lett)
This result was superior to the second-line treatment with nab-paclitaxel, which resulted in a PFS of 8 months and best overall response of stable disease with slight shrinkage. The present case indicates that a combination of utidelone with apatinib/anlotinib exhibited antitumor activity in a patient with HR+/HER2- mBC with BMs. Therefore, this combination offers a promising therapeutic option for the clinical treatment of patients with breast cancer and BMs.
Journal
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HER-2 (Human epidermal growth factor receptor 2)
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HR positive • HER-2 negative
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Focus V (anlotinib) • AiTan (rivoceranib) • albumin-bound paclitaxel • utidelone IV (UTD1)
3d
New P2 trial • Metastases
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CLDN6 (Claudin 6) • PROC (Protein C, Inactivator Of Coagulation Factors Va And VIIIa)
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CLDN6 expression
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TORL-1-23 • Neulasta (pegfilgrastim)
3d
Phase 2 Trial of Enfortumab Vedotin in Patients With Previously Treated Locally Advanced or Metastatic Urothelial Carcinoma in China. (PubMed, Cancer Med)
Enfortumab vedotin demonstrated meaningful clinical activity with a manageable safety profile in Chinese patients with previously treated locally advanced or mUC.
P2 data • Journal • Metastases
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NECTIN4 (Nectin Cell Adhesion Molecule 4)
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Padcev (enfortumab vedotin-ejfv)
4d
Phase Ib clinical and pharmacodynamic study of the TIE2 kinase inhibitor rebastinib with paclitaxel or eribulin in HER2-negative metastatic breast cancer. (PubMed, Clin Cancer Res)
In patients with MBC, the recommended phase 2 dose of rebastinib associated with pharmacodynamic evidence of TIE2 inhibition is either 50 or 100 mg PO BID in combination with paclitaxel or eribulin.
P1 data • PK/PD data • Journal • Metastases
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HER-2 (Human epidermal growth factor receptor 2)
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HER-2 negative
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paclitaxel • Halaven (eribulin mesylate) • rebastinib (DCC-2036)
4d
A case report of interstitial lung disease caused by HER2-positive breast cancer patient receiving two antibody-drug conjugate drugs successively. (PubMed, Transl Breast Cancer Res)
The patient was treated with ADCs of ARX-788 for third-line treatment, she had ILD. After treatment of ILD, the patient was treated with ADCs of trastuzumab-DM1 (T-DM1) for fourth-line treatment and she had ILD again...Whether other anti-HER2 ADCs can be tried in the later lines is still being cautious. Whether there is a certain relationship between the side effects and efficacy of ADCs, there is no evidence-based data.
Journal
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HER-2 (Human epidermal growth factor receptor 2)
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HER-2 positive • EGFR positive
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Kadcyla (ado-trastuzumab emtansine) • anvatabart opadotin (JNJ-0683)
5d
KEYNOTE-E02: Efficacy and Safety Study of Tisotumab Vedotin for Patients With Solid Tumors (clinicaltrials.gov)
P2, N=692, Recruiting, Seagen Inc. | Trial primary completion date: Apr 2025 --> Feb 2026
Trial primary completion date
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PD-L1 (Programmed death ligand 1)
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PD-L1 expression
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Keytruda (pembrolizumab) • cisplatin • carboplatin • Tivdak (tisotumab vedotin-tftv)
5d
A Study of MORAb-202 in Participants With Previously Treated Metastatic Non-Small Cell Lung Cancer (NSCLC) Adenocarcinoma (AC) (clinicaltrials.gov)
P2, N=50, Terminated, Bristol-Myers Squibb | Trial completion date: Feb 2026 --> Aug 2024 | Recruiting --> Terminated | Trial primary completion date: Mar 2024 --> Aug 2024; Business objectives have changed
Trial completion date • Trial termination • Trial primary completion date • Metastases
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farletuzumab ecteribulin (MORAb-202)
5d
SGNB7H4V-001: A Study of SGN-B7H4V in Advanced Solid Tumors (clinicaltrials.gov)
P1, N=572, Recruiting, Seagen Inc. | N=430 --> 572 | Trial completion date: Jan 2027 --> Nov 2027 | Trial primary completion date: Jun 2025 --> Nov 2027
Enrollment change • Trial completion date • Trial primary completion date
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HER-2 (Human epidermal growth factor receptor 2)
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HR positive • HER-2 negative • PTEN mutation + HR positive
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Keytruda (pembrolizumab) • felmetatug vedotin (PF-08046048)
6d
New P2 trial
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Avastin (bevacizumab) • utidelone IV (UTD1)
6d
Enrollment open
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luveltamab tazevibulin (STRO-002)
6d
A Study of the ILB-3101 in Patients With Advanced Solid Tumors (clinicaltrials.gov)
P1, N=240, Recruiting, Innolake Biopharm | Not yet recruiting --> Recruiting | Initiation date: Aug 2024 --> Oct 2024
Enrollment open • Trial initiation date • Metastases
8d
A study Disitamab Vedotin Plus Trastuzumab in Patients With HER2 Positive GC/GEJ Patiens (ChiCTR2400088975)
P1/2, N=35, Not yet recruiting, Zhejiang Cancer Hospital; Zhejiang Cancer Hospital
New P1/2 trial
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HER-2 positive
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Herceptin (trastuzumab) • Aidixi (disitamab vedotin)
10d
Enrollment closed • Enrollment change • Combination therapy
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SDC1 (Syndecan 1)
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pomalidomide • Blenrep (belantamab mafodotin-blmf) • Ogsiveo (nirogacestat)
10d
R-Pola-Glo: Rituximab in Combination with Glofitamab and Polatuzumab Vedotin in Patients with Previously Untreated Aggressive B-cell Lymphoma Ineligible for R-CHOP (clinicaltrials.gov)
P2, N=125, Recruiting, Institut für Klinische Krebsforschung IKF GmbH at Krankenhaus Nordwest | Active, not recruiting --> Recruiting | N=80 --> 125 | Trial primary completion date: Sep 2027 --> Apr 2025
Enrollment open • Enrollment change • Trial primary completion date • Combination therapy
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Rituxan (rituximab) • Gazyva (obinutuzumab) • Polivy (polatuzumab vedotin-piiq) • Columvi (glofitamab-gxbm)
10d
A Phase 2 Study of Mirvetuximab Soravtansine (IMGN853) and Pembrolizumab in Endometrial Cancer (EC) (clinicaltrials.gov)
P2, N=18, Active, not recruiting, Dana-Farber Cancer Institute | Trial completion date: Aug 2028 --> May 2027 | Trial primary completion date: Aug 2025 --> Jun 2024
Trial completion date • Trial primary completion date • Combination therapy
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FOLR1 ( Folate receptor alpha ) • MLH1 (MutL homolog 1) • MSH6 (MutS homolog 6) • MSH2 (MutS Homolog 2)
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MSH6 expression
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Keytruda (pembrolizumab) • Elahere (mirvetuximab soravtansine-gynx)
11d
Enrollment open • Combination therapy • Metastases
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Avastin (bevacizumab) • luveltamab tazevibulin (STRO-002)
11d
New P2 trial
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Halaven (eribulin mesylate)
11d
New P1/2 trial
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luveltamab tazevibulin (STRO-002)
12d
Risk Classification of Patients With Advanced Urothelial Carcinoma Treated With Enfortumab Vedotin. (PubMed, Cancer Diagn Progn)
Significant differences were observed in PFS and OS among the three groups (p<0.001 and p<0.001, respectively) and c-indices were 0.766 for PFS and 0.800 for OS. The risk classification using CRP and hypercalcemia is useful for predicting the outcomes of patients with advanced UC treated with EV.
Journal • Metastases
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CRP (C-reactive protein)
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Padcev (enfortumab vedotin-ejfv)
12d
Brentuximab Vedotin and Nivolumab in Treating Patients With Early Stage Classic Hodgkin Lymphoma (clinicaltrials.gov)
P2, N=155, Active, not recruiting, City of Hope Medical Center | Trial completion date: Sep 2024 --> Dec 2024 | Trial primary completion date: Sep 2024 --> Dec 2024
Trial completion date • Trial primary completion date
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Opdivo (nivolumab) • doxorubicin hydrochloride • Adcetris (brentuximab vedotin) • dacarbazine • daunorubicin • bleomycin • vinblastine
12d
Belantamab Mafodotin As Pre- and Post-Autologous Stem Cell Transplant (ASCT) Consolidation and Maintenance for Multiple Myeloma (MM) with < Complete Response after Induction: Interim Results of the Ongoing Phase 2 BLAST Study (ASH 2024)
Background: High dose melphalan and ASCT, followed by lenalidomide (len) maintenance, improves progression-free survival (PFS) in MM but is generally not curative. In newly-diagnosed MM patients with <CR after induction, belamaf every 3 months in conjunction with ASCT and len maintenance appears feasible (at 1.9 mg/kg starting dose), with expected reversible ocular toxicities, and so far has promising rates of sCR, MRD-negativity, and PFS. Accrual and follow-up are ongoing.
Clinical • P2 data • IO biomarker
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CD34 (CD34 molecule)
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clonoSEQ
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lenalidomide • melphalan • Blenrep (belantamab mafodotin-blmf)
12d
Unveiling the future of breast cancer therapy: Cutting-edge antibody-drug conjugate strategies and clinical outcomes. (PubMed, Breast)
For the treatment of breast cancer, there are three ADCs approved for breast cancer treatment: Trastuzumab emtansine (T-DM1), Trastuzumab Deruxtecan (T-Dxd) targeting HER-2, and Sacituzumab Govitecan (SG) targeting Trop-2. This review summarizes the efficacy and adverse effects of ADC therapies that have completed or are currently undergoing phase I-III clinical trials. Additionally, it analyzes potential combination strategies to overcome ADC resistance, aiming to provide clinicians with a comprehensive clinical guide to the use of ADCs in breast cancer treatment.
Clinical data • Review • Journal
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HER-2 (Human epidermal growth factor receptor 2)
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HER-2 positive • HR positive • HER-2 expression • HER-2 underexpression
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Kadcyla (ado-trastuzumab emtansine) • Enhertu (fam-trastuzumab deruxtecan-nxki) • Trodelvy (sacituzumab govitecan-hziy)
13d
Hepatopulmonary syndrome associated with long-term use of ado-trastuzumab emtansine (T-DM1) for treatment of HER2-positive metastatic breast cancer - a case report and series. (PubMed, Front Oncol)
The emergence of dyspnea alone or combined with low oxygen saturation and signs of hypoxemia (clubbing or elevated hemoglobin) should raise clinical suspicion and prompt evaluation for HPS. Cancer care team members should be vigilant regarding the potential for new and serious side effects associated with novel targeted therapies, which may emerge years beyond initial regulatory approval.
Journal • Metastases
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HER-2 (Human epidermal growth factor receptor 2)
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HER-2 positive
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Kadcyla (ado-trastuzumab emtansine)
13d
A Study of Polatuzumab Vedotin, Rituximab and Dose Attenuated CHP in Older Patients with DLBCL (clinicaltrials.gov)
P2, N=39, Recruiting, University of Rochester | Trial completion date: Jul 2024 --> Jul 2026 | Trial primary completion date: Jul 2024 --> Jul 2026
Trial completion date • Trial primary completion date
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MYC (V-myc avian myelocytomatosis viral oncogene homolog) • BCL2 (B-cell CLL/lymphoma 2) • BCL6 (B-cell CLL/lymphoma 6)
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BCL6 rearrangement • BCL2 rearrangement
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Rituxan (rituximab) • doxorubicin hydrochloride • cyclophosphamide • prednisone • Polivy (polatuzumab vedotin-piiq)
13d
E7389-J081-114: Study of E7389 Liposomal Formulation in Participants With Solid Tumor (clinicaltrials.gov)
P1, N=140, Active, not recruiting, Eisai Co., Ltd. | Trial completion date: Aug 2025 --> Mar 2026
Trial completion date
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HER-2 (Human epidermal growth factor receptor 2) • PD-L1 (Programmed death ligand 1)
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HER-2 negative • PD-L1 negative
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eribulin liposomal (E7389-LF)
13d
A Study of E7130 in Participants With Solid Tumors (clinicaltrials.gov)
P1, N=95, Active, not recruiting, Eisai Co., Ltd. | Trial completion date: Jun 2025 --> Jun 2026 | Trial primary completion date: Jun 2025 --> Jun 2026
Trial completion date • Trial primary completion date
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E7130
14d
Enrollment change
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MET (MET proto-oncogene, receptor tyrosine kinase)
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MET amplification • MET exon 14 mutation • MET mutation
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MYTX-011
17d
Trial completion date
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CEACAM5 (CEA Cell Adhesion Molecule 5)
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docetaxel • tusamitamab ravtansine (SAR408701)
17d
NCI-2021-12489: Mosunetuzumab With or Without Polatuzumab Vedotin and Obinutuzumab for the Treatment of Untreated Indolent B-Cell Non-Hodgkin Lymphoma (clinicaltrials.gov)
P2, N=42, Active, not recruiting, University of Washington | Recruiting --> Active, not recruiting | Trial completion date: Dec 2025 --> Mar 2025 | Trial primary completion date: Dec 2025 --> Mar 2025
Enrollment closed • Trial completion date • Trial primary completion date
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Gazyva (obinutuzumab) • Polivy (polatuzumab vedotin-piiq) • Lunsumio (mosunetuzumab-axgb)
18d
Trial completion date • Trial primary completion date
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HER-2 (Human epidermal growth factor receptor 2) • BRAF (B-raf proto-oncogene) • ER (Estrogen receptor) • ALK (Anaplastic lymphoma kinase) • PGR (Progesterone receptor) • ROS1 (Proto-Oncogene Tyrosine-Protein Kinase ROS)
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HER-2 negative • PGR negative
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prednisone • dexamethasone • farletuzumab ecteribulin (MORAb-202) • prednisolone
18d
OSU-17204: Brentuximab Vedotin and Lenalidomide in Treating Patients With Stage IB-IVB Relapsed or Refractory T-Cell Lymphoma (clinicaltrials.gov)
P2, N=26, Active, not recruiting, John Reneau | Trial completion date: Apr 2024 --> May 2025 | Trial primary completion date: Apr 2024 --> May 2025
Trial completion date • Trial primary completion date
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TNFRSF8 (TNF Receptor Superfamily Member 8)
|
TNFRSF8 positive
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lenalidomide • Adcetris (brentuximab vedotin)
18d
Safety and Preliminary Efficacy of JBH492 Monotherapy in Patients With CLL and NHL (clinicaltrials.gov)
P1, N=25, Terminated, Novartis Pharmaceuticals | Active, not recruiting --> Terminated; Business, strategic, and development considerations and not due to any safety concerns
Trial termination
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JBH492
18d
New P1/2 trial • Metastases
18d
Structural insights into epitope-paratope interactions of a monoclonal antibody targeting CEACAM5-expressing tumors. (PubMed, Nat Commun)
The antibody-drug conjugate tusamitamab ravtansine specifically recognizes the A3-B3 domains of human CEACAM5 (hCEACAM5)...The cryogenic electron microscopy structure of the hCEACAM5A3-B3- tusa Fab complex (3.11 Å overall resolution) reveals a discontinuous epitope involving residues in the A3-B3 domains and an N-linked mannose at residue Asn612. Conformational constraints on the epitope-paratope interface enable tusamitamab to target hCEACAM5A3-B3 and distinguish CEACAM5 from other CEACAMs.
Journal
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CEACAM5 (CEA Cell Adhesion Molecule 5)
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CEACAM5 expression
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tusamitamab ravtansine (SAR408701)