^
Contact us  to learn more about
our Premium Content:  News alerts, weekly reports and conference planners
DRUG CLASS:

Bcl2 inhibitor

Related drugs:
1d
Aprepitant mitigates paclitaxel-induced neuropathic pain in rats via suppressing inflammatory pathways in dorsal root ganglia. (PubMed, Drug Chem Toxicol)
Aprepitant was orally administered every alternate day between days 2 and 14, with a prescribed dosage of 10 or 20 mg/kg. In addition, aprepitant application suppressed the protein expression of NF-kB in the dorsal root ganglia of paclitaxel-treated rats, as revealed by western blot analysis. Aprepitant treatment ameliorates neuropathy induced by paclitaxel, which is associated with decreasing proinflammatory cytokines and NF-kB expression.
Preclinical • Journal
|
TNFA (Tumor Necrosis Factor-Alpha) • NFKB1 (Nuclear factor of kappa light polypeptide gene enhancer in B-cells 1) • IL1B (Interleukin 1, beta)
|
NFKB1 expression
|
paclitaxel • aprepitant oral
1d
Microtubule poleward flux as a target for modifying chromosome segregation errors. (PubMed, Proc Natl Acad Sci U S A)
In a similar manner, a low-dose taxol treatment rescued mitotic errors in a high-grade serous ovarian carcinoma cell line OVKATE. Collectively, our results highlight the potential of targeting microtubule poleward flux to modify chromosome instability and provide insight into the mechanism through which low doses of taxol rescue certain mitotic errors in cancer cells.
Journal
|
KIF18A (Kinesin Family Member 18A)
|
paclitaxel
2d
Cocrystal@protein-anchoring nanococktail for combinatorially treating multidrug-resistant cancer. (PubMed, Acta Pharm Sin B)
Herein, a "one stone and three birds" nanococktail integrated by a cocrystal@protein-anchoring strategy was purposed for triple-payload delivery, which paclitaxel-disulfiram cocrystal-like nanorods (NRs) were anchored with the basic protein drug Cytochrome c (Cyt C), followed by hyaluronic-acid modification. Our mechanistic study indicated that the system induced the apoptosis of Taxol-resistant tumor cells through the signal axis P-glycoprotein/Cyt C/caspase 3. Collectively, this nanococktail strategy offers a promising approach to improve the sensitivity of tumor cells to chemotherapeutic drugs and strengthen intractable drug-resistant oncotherapy.
Journal
|
CASP3 (Caspase 3)
|
paclitaxel
2d
Multi-omics analysis revealed significant metabolic changes in brain cancer cells treated with paclitaxel and/or topotecan. (PubMed, Heliyon)
Overall, this study underscores the effectiveness of multi-omics approaches in revealing the molecular mechanisms driving chemotherapy responses in cancer cells. Additionally, this work generates a comprehensive list of molecular alterations that can serve as a foundation for further investigations and inform personalized healthcare strategies to enhance patient outcomes.
Journal
|
HIF1A (Hypoxia inducible factor 1, alpha subunit) • RACK1 (Receptor For Activated C Kinase 1) • RPA3 (Replication Protein A3)
|
paclitaxel • topotecan
3d
Targeted Elimination of the Oral Pathogen to Overcome Chemoresistance of Oral Squamous Cell Carcinoma by Biologically Derived Nanotherapeutics. (PubMed, ACS Nano)
Accordingly, the biologically derived nanovesicles from ginger (GDNVs) with excellent P. gingivalis elimination ability are explored to transport the clinically used drug paclitaxel (PTX) for potentiating the therapeutic efficiency...By evaluating both P. gingivalis-infected tumor cells and P. gingivalis-infiltrated tumor-bearing mice, P-GDNVs show a much enhanced tumor cell killing effect, as compared with free PTX. This naturally occurring nanotherapeutic system represents an effective bioactive material for targeted elimination of host microbiota to boost therapeutic response, showing great promise to combat commensal microbiota-rich tumors.
Journal
|
IL6 (Interleukin 6)
|
paclitaxel
3d
Soybean β-Conglycinin and Cowpea β-Vignin Peptides Inhibit Breast and Prostate Cancer Cell Growth: An In Silico and In Vitro Approach. (PubMed, Foods)
The VIPAAY peptide from the soybean β-conglycinin β subunit showed the highest potential to interact with Bcl-2, comparable to Venetoclax, a well-known anticancer drug. Further experiments are needed to confirm this study's findings.
Preclinical • Journal
|
BCL2 (B-cell CLL/lymphoma 2)
|
Venclexta (venetoclax)
3d
Oncogene Downregulation by Mahanine Suppresses Drug-Sensitive and Drug-Resistant Lung Cancer and Inhibits Orthotopic Tumor Progression. (PubMed, Cancers (Basel))
The antiproliferative activity of MH was determined using MTT and colony formation assays against drug-sensitive (A549 and H1299) and Taxol-resistant lung cancer cells (A549-TR)...In vivo, MH (25 mg/kg b. wt.) significantly (p < 0.001) inhibited the growth of A549 lung cancer orthotopic xenografts in NOD Scid mice by 70%. Our study provides new mechanistic insights into MH's therapeutic potential against NSCLC.
Journal • IO biomarker
|
MYC (V-myc avian myelocytomatosis viral oncogene homolog) • BCL2 (B-cell CLL/lymphoma 2) • CDK4 (Cyclin-dependent kinase 4) • BCL2L1 (BCL2-like 1) • BIRC5 (Baculoviral IAP repeat containing 5) • CDK1 (Cyclin-dependent kinase 1)
|
paclitaxel
3d
NCI-2013-02103: Testing the Addition of Navitoclax to the Combination of Dabrafenib and Trametinib in People Who Have BRAF Mutant Melanoma (clinicaltrials.gov)
P1/2, N=75, Active, not recruiting, National Cancer Institute (NCI) | Trial completion date: Dec 2024 --> Dec 2025 | Trial primary completion date: Dec 2024 --> Dec 2025
Trial completion date • Trial primary completion date • IO biomarker
|
PTEN (Phosphatase and tensin homolog) • BCL2 (B-cell CLL/lymphoma 2)
|
BRAF V600E • BRAF mutation • BRAF V600 • PTEN mutation • BRAF V600K
|
THXID® BRAF Kit • cobas® 4800 BRAF V600 Mutation Test
|
Mekinist (trametinib) • Tafinlar (dabrafenib) • navitoclax (ABT 263) • omipalisib (GSK2126458)
3d
Decitabine and Venetoclax Treatment as Maintenance Therapy in Patients Post Allograft Stem Cell Transplant (clinicaltrials.gov)
P1/2, N=20, Not yet recruiting, Benjamin Tomlinson | Trial completion date: Dec 2025 --> Dec 2026 | Trial primary completion date: Dec 2024 --> Dec 2025
Trial completion date • Trial primary completion date
|
BCL2 (B-cell CLL/lymphoma 2)
|
Venclexta (venetoclax) • decitabine
3d
New trial • Metastases
|
albumin-bound paclitaxel • irinotecan
4d
Antineoplastic therapy affects the in vitro phenotype and functionality of healthy human bone marrow-derived mesenchymal stromal cells. (PubMed, Arch Toxicol)
To address this, we investigated the effects of etoposide, temozolomide, 5-azacitidine, and venetoclax on healthy BM-derived MSC functionality. Our findings show that besides HSPC, also MSC are sensitive to certain antineoplastic agents, resulting in molecular and functional alterations that may contribute to therapy-related myelosuppression. Understanding these interactions could be helpful for the development of strategies to preserve BM MSC functionality during different kinds of anticancer therapies.
Preclinical • Journal • Stroma
|
CDKN1A (Cyclin-dependent kinase inhibitor 1A)
|
Venclexta (venetoclax) • temozolomide • azacitidine • etoposide IV
4d
Homoharringtonine Added to Venetoclax and Azacitidine Improves Outcome and Mitigates Genetic Impact in Relapsed/Refractory AML: A Multi-center Cohort Study. (PubMed, Clin Cancer Res)
Our findings suggest the addition of HHT to VA might enhance response and mitigate the negative impact of certain genetic patterns in RR-AML while being well tolerated.
Journal
|
KRAS (KRAS proto-oncogene GTPase) • FLT3 (Fms-related tyrosine kinase 3) • NPM1 (Nucleophosmin 1) • DNMT3A (DNA methyltransferase 1) • TET2 (Tet Methylcytosine Dioxygenase 2)
|
KRAS mutation • FLT3-ITD mutation • FLT3 mutation • DNMT3A mutation • TET2 mutation
|
Venclexta (venetoclax) • azacitidine • Synribo (omacetaxine mepesuccinate)
4d
SA-002804: A Study to Evaluate the Efficacy and Safety of Obinutuzumab, Ibrutinib, and Venetoclax in Patients With Richter's Syndrome; (clinicaltrials.gov)
P2, N=15, Active, not recruiting, Bnai Zion Medical Center | Recruiting --> Active, not recruiting | Trial primary completion date: Mar 2024 --> Dec 2024
Enrollment closed • Trial primary completion date
|
Venclexta (venetoclax) • Imbruvica (ibrutinib) • Gazyva (obinutuzumab)
5d
Venetoclax and Azacitidine for Non-Elderly Adult Patients With Acute Myeloid Leukemia (clinicaltrials.gov)
P2, N=36, Active, not recruiting, University of Colorado, Denver | Recruiting --> Active, not recruiting
Enrollment closed
|
Venclexta (venetoclax) • azacitidine
5d
Demethylating Agents Combined with Venetoclax for High-risk T-Cell Lymphoma/leukemia Post-Transplant Relapse Prevention (clinicaltrials.gov)
P2, N=59, Recruiting, Shanghai General Hospital, Shanghai Jiao Tong University School of Medicine
New P2 trial • Post-transplantation
|
Venclexta (venetoclax) • azacitidine • decitabine
6d
New P2 trial • Metastases
|
cisplatin • albumin-bound paclitaxel • cyclophosphamide • ifosfamide
6d
Enrollment open
|
Venclexta (venetoclax) • cytarabine
8d
New trial
|
Venclexta (venetoclax) • azacitidine • Synribo (omacetaxine mepesuccinate)
8d
New trial • Combination therapy • Real-world evidence • Real-world
|
Venclexta (venetoclax)
8d
Risk-stratified treatment of sonrotoclax combined with chemotherapy in patients with newly diagnosed acute myeloid leukemia: a multicenter, phase II stud (ChiCTR2400090001)
P=N/A, N=47, Not yet recruiting, Ruijin Hospital, Shanghai Jiao Tong University School of Medicine; Ruijin Hospital, Shanghai Jiao Tong University School of Medicine
New trial
|
sonrotoclax (BGB-11417)
8d
New trial
|
PML (Promyelocytic Leukemia)
|
Venclexta (venetoclax) • Intron A (interferon α-2b)
8d
Real world data to evaluate the efficacy of paclitaxel plus cisplatin in the treatment of breast cancer (ChiCTR2400089679)
P=N/A, N=304, Not yet recruiting, Renji Hospital affiliated to Shanghai Jiaotong University School of Medicine; Renji Hospital affiliated to Shanghai Jiaotong University School of Medi
New trial • Real-world evidence • Real-world
|
cisplatin • paclitaxel
8d
New trial
|
PML (Promyelocytic Leukemia)
|
PML-RARA fusion
|
Venclexta (venetoclax) • idarubicin hydrochloride
8d
New P4 trial
|
FLT3 (Fms-related tyrosine kinase 3)
|
FLT3 mutation
|
Venclexta (venetoclax) • cytarabine
8d
A prospective, single-center, single-arm study of mitoxantrone hydrochloride liposome injection combined with venetoclax and azacitidine in the treatment of newly diagnosed and relapsed/refractory acute myeloid leukemia (ChiCTR2400091259)
P4, N=40, Not yet recruiting, General Hospital of Chinese People's Liberation Army Northern Theater Command; General Hospital of Chinese People's Liberation Army Northern Theater C
New P4 trial
|
Venclexta (venetoclax) • azacitidine • Duoenda (mitoxantrone liposomal)
8d
New P4 trial • Metastases
|
gemcitabine • albumin-bound paclitaxel
8d
New P2 trial • Combination therapy • Metastases
|
carboplatin • paclitaxel
8d
New P2 trial
|
Venclexta (venetoclax) • cytarabine
10d
ENABLE: Trial in AML Secondary to MPNs Patients, Unfit for Intensive Chemotherapy, Investigating a Treatment Combination Including Decitabine and Venetoclax (clinicaltrials.gov)
P2, N=101, Active, not recruiting, Gruppo Italiano Malattie EMatologiche dell'Adulto | Recruiting --> Active, not recruiting | Trial completion date: May 2024 --> Apr 2026 | Trial primary completion date: May 2024 --> Oct 2024
Enrollment closed • Trial completion date • Trial primary completion date
|
Venclexta (venetoclax) • decitabine
11d
Prognosis prediction of head and neck squamous cell carcinoma through the basement membrane-related lncRNA risk model. (PubMed, Front Mol Biosci)
Additionally, heightened sensitivity to paclitaxel and docetaxel was evident in the patients at high risk. We have established a BMLncRNA-based prognostic model that can provide clinical guidance for future laboratory and clinical studies of HNSCC.
Journal • Tumor mutational burden • IO biomarker
|
TMB (Tumor Mutational Burden)
|
paclitaxel • docetaxel
11d
PALVEN: Palbociclib, Letrozole & Venetoclax in ER and BCL-2 Positive Breast Cancer (clinicaltrials.gov)
P1, N=17, Active, not recruiting, Peter MacCallum Cancer Centre, Australia | Trial primary completion date: Jun 2024 --> Jun 2025
Trial primary completion date • Metastases
|
HER-2 (Human epidermal growth factor receptor 2) • ER (Estrogen receptor) • BCL2 (B-cell CLL/lymphoma 2)
|
ER positive • HER-2 negative • BCL2 positive • HER-2 negative + ER positive
|
Venclexta (venetoclax) • Ibrance (palbociclib) • letrozole
11d
Trial suspension • Combination therapy
|
Venclexta (venetoclax)
12d
Minimal Residual Disease Testing in Relapsed Systemic AL Amyloidosis (ASH 2024)
Background The only FDA-approved therapy for systemic light chain (AL) amyloidosis is daratumumab plus cyclophosphamide, bortezomib, and dexamethasone (i.e., Dara-CyBorD)...At the time of the MRD test, 30 (58.8%) patients were on active surveillance, 10 (19.6%) were on daratumumab and 9 (17.6%) on venetoclax...In patients with relapsed AL, MRD negativity is correlated with a better hematological response and could potentially play a role in clinical trial design. The impact of gender on MRD status remains an important area for further study.
Minimal residual disease
|
clonoSEQ
|
Venclexta (venetoclax) • bortezomib • cyclophosphamide • dexamethasone • Darzalex Faspro (daratumumab and hyaluronidase-fihj)
12d
Preliminary Efficacy and Safety of a Phase 1/2 Study of Acalabrutinib, Venetoclax, and Obinutuzumab in Patients with Relapsed/Refractory and Previously Untreated Mantle Cell Lymphoma (MAVO) (ASH 2024)
The combination of the Bruton tyrosine kinase inhibitor (BTKi) ibrutinib, the BCL-2 inhibitor venetoclax (V), and the anti-CD20 monoclonal antibody (mAb) obinutuzumab (O) has demonstrated safety and efficacy in R/R and TN MCL (Le Gouill, Blood 2021). AVO is safe and active in pts with R/R and TP53-aberrant/transplant ineligible TN MCL. Preliminary efficacy and feasibility of an MRD-guided treatment approach is encouraging in this high-risk TN cohort B. Our data supports further investigation of a targeted triplet approach, and the phase II TN transplant eligible and TP53 wild type cohort is enrolling based on demonstrated safety and efficacy in cohort B. Updated results will be presented at the meeting.
Clinical • P1/2 data • IO biomarker
|
TP53 (Tumor protein P53)
|
TP53 mutation • TP53 wild-type • TP53 expression
|
clonoSEQ
|
Venclexta (venetoclax) • Imbruvica (ibrutinib) • Gazyva (obinutuzumab) • Calquence (acalabrutinib)
12d
Primary Endpoint Evaluation of a Multicenter, Phase 2 Study of Acalabrutinib, Venetoclax, Obinutuzumab (AVO) in a Population of Previously Untreated Patients with CLL Enriched for High-Risk Disease (ASH 2024)
Responses are durable, with 89%, 87%, and 77% 4-yr PFS in all-comer, uIGHV, and TP53 aberrant pts. Our data support further study of AVO for pts with TN high risk CLL in GCLLSG CLL16 and future trials.
Clinical • P2 data • IO biomarker
|
TP53 (Tumor protein P53) • BCL2 (B-cell CLL/lymphoma 2) • NOTCH1 (Notch 1) • IGH (Immunoglobulin Heavy Locus)
|
TP53 mutation • NOTCH1 mutation
|
clonoSEQ
|
Venclexta (venetoclax) • Gazyva (obinutuzumab) • Calquence (acalabrutinib)
12d
Multicenter Phase II Trial of Zanubrutinib, Obinutuzumab, and Venetoclax (BOVen) in Treatment-Naïve Chronic Lymphocytic Leukemia: 5-Year Follow up, Retreatment Outcomes, and Impact of MRD Kinetics (ΔMRD400) (ASH 2024)
Zanubrutinib is a second-generation BTKi with superior PFS and safety compared with ibrutinib (Brown NEJM 2023). Five-year follow up of the BOVen regimen demonstrates frequent uMRD4 in PB (96%) and BM (92%), and uMRD4 was durable with a median MRD4-free survival of 34 mo. Retreatment with zanubrutinib-venetoclax was also well-tolerated and effective. A phase 2 trial of BOVen with ΔMRD400-directed treatment duration is ongoing.
Clinical • P2 data
|
clonoSEQ
|
Venclexta (venetoclax) • Imbruvica (ibrutinib) • Gazyva (obinutuzumab) • Brukinsa (zanubrutinib)
12d
Real World Experience with Time Limited Venetoclax and Obinutuzumab (VO) for Frontline Treatment of CLL/SLL with MRD Determination By Clonoseq® (ASH 2024)
VO is highly effective and feasible in both academic and community settings. The ability of obi to debulk patients prior to ven initiation allowed most patients to receive ven initiation in the outpatient setting. TLS is rare and was only seen secondary to obi.
Clinical • Real-world evidence • Real-world
|
clonoSEQ
|
Venclexta (venetoclax) • Gazyva (obinutuzumab)
12d
Results from a Clinical Study of the All-Oral Regimen of CC-486 (Oral Azacitidine) and Venetoclax for Newly Diagnosed and Relapsed and Refractory Acute Myeloid Leukemia (ASH 2024)
Background: Venetoclax (ven) with azacitidine (aza) is the standard of care for newly diagnosed AML patients who are unfit for intensive induction chemotherapy. CC-486 (oral azacitidine) and ven is an all-oral regimen currently being investigated for the treatment of ND and R/R AML. The phase I portion of this study previously showed the MTD of CC-486 with ven to be 300mg d1-14 (Amaya et al. 2023).
Clinical
|
TP53 (Tumor protein P53)
|
Venclexta (venetoclax) • Onureg (azacitidine oral)
12d
IDH2 Mutation Is Associated with Favorable Outcome Among Older Adults with Newly Diagnosed Acute Myeloid Leukemia Treated with Lower-Intensity Therapy (ASH 2024)
Among the LIT treated patients, 96 patients received treatment with an IDH inhibitor, and 237 patients received a hypomethylating agent (HMA) plus venetoclax... A total of 1023 patients with ND AML were identified. Patients had a median age of 72 (range 60-92) years and the majority were non-Hispanic White (83.2%), and male (57.6%). Ninety-nine (9.7%) patients were IDH1MUT, 193 (18.9%) patients were IDH2MUT including 10 (1.0%) patients with a co-occurring IDH1 and IDH2 gene mutations.
Clinical
|
IDH1 (Isocitrate dehydrogenase (NADP(+)) 1) • IDH2 (Isocitrate Dehydrogenase (NADP(+)) 2) • DNMT3A (DNA methyltransferase 1) • SRSF2 (Serine and arginine rich splicing factor 2)
|
IDH2 mutation • NPM1 mutation
|
FoundationOne® Heme CDx
|
Venclexta (venetoclax)
12d
Phase 1b/2 Study of Venetoclax, Ibrutinib, Prednisone, Obinutuzumab, and Lenalidomide (ViPOR) in Relapsed/Refractory and Treatment-Naïve Mantle Cell Lymphoma: Preliminary Analysis of Safety, Efficacy, and Minimal Residual Disease (ASH 2024)
Fixed-duration ViPOR x 6C without maintenance achieved CR in 100% and uMRD in 97% of MCL pts, with ongoing CR in 95% and 73% of TN and R/R pts, respectively, and only 1 R/R pt receiving consolidative allo-HSCT. This includes blastoid, TP53 mutated, and post-BTKi high-risk subsets. ViPOR with a 12d VEN ramp-up on C2 is safe in MCL pts of all ages without significant TLS or febrile neutropenia.
Clinical • P1/2 data • Minimal residual disease
|
TP53 (Tumor protein P53) • CD20 (Membrane Spanning 4-Domains A1)
|
TP53 mutation • TP53 expression
|
clonoSEQ
|
Venclexta (venetoclax) • Imbruvica (ibrutinib) • lenalidomide • Gazyva (obinutuzumab) • prednisone