Discovery and Development of Dolastatin 10-Derived Antibody Drug Conjugate Anticancer Drugs

Natural Product Based Antibody Drug Conjugates: Clinical Status as of November 9, 2020

(2021) David J. Newman   JOURNAL OF NATURAL PRODUCTS

A Novel c-MET-Targeting Antibody-Drug Conjugate for Pancreatic Cancer

(2021) Yangbing Jin et al.   Frontiers in Oncology

First-in-Human Study of PF-06647020 (Cofetuzumab Pelidotin), an Antibody–Drug Conjugate Targeting Protein Tyrosine Kinase 7, in Advanced Solid Tumors

(2021) Michael L. Maitland et al.   CLINICAL CANCER RESEARCH

Safety and unique pharmacokinetic profile of ARX788, a site-specific ADC, in heavily pretreated patients with HER2-overexpresing solid tumors: Results from two phase 1 clinical trials.

(2021) Sara A. Hurvitz et al.   JOURNAL OF CLINICAL ONCOLOGY

Phase I study of A166 in patients with HER2-expressing locally advanced or metastatic solid tumors.

(2021) Xichun Hu et al.   JOURNAL OF CLINICAL ONCOLOGY

A phase 1 multicenter, dose expansion study of ARX788 as monotherapy in patients with HER2-positive advanced gastric and gastroesophageal junction adenocarcinoma (ACE-Gastric-01).

(2021) Yang Zhang et al.   JOURNAL OF CLINICAL ONCOLOGY

Marine Antitumor Peptide Dolastatin 10: Biological Activity, Structural Modification and Synthetic Chemistry

(2021) Gang Gao et al.   Marine Drugs

Discovery of Dolastatinol: A Synthetic Analog of Dolastatin 10 and Low Nanomolar Inhibitor of Tubulin Polymerization

(2021) Hodaya Gutman et al.   ACS Medicinal Chemistry Letters

A phase I dose escalation study evaluating the safety and tolerability of a novel anti-HER2 antibody-drug conjugate (PF-06804103) in patients with HER2-positive solid tumors.

(2020) Funda Meric-Bernstam et al.   JOURNAL OF CLINICAL ONCOLOGY

Antineoplastic Agents. 607. Emetine Auristatins

(2020) George R. Pettit et al.   JOURNAL OF NATURAL PRODUCTS

Nonclinical Development of Next Generation Site-Specific HER2 Targeting Antibody Drug Conjugate (ARX788) for Breast Cancer Treatment

(2020) Prathap Nagaraja Shastri et al.   MOLECULAR CANCER THERAPEUTICS

ARX788, a Site-specific anti-HER2 Antibody Drug Conjugate, Demonstrates Potent and Selective Activity in HER2 Low and T-DM1 Resistant Breast and Gastric Cancers

(2020) Lillian Skidmore et al.   MOLECULAR CANCER THERAPEUTICS

PF-06804103, a site-specific anti-HER2 antibody-drug conjugate for the treatment of HER2-expressing breast, gastric, and lung cancers

(2020) Edmund I. Graziani et al.   MOLECULAR CANCER THERAPEUTICS

Belantamab Mafodotin: First Approval

(2020) Anthony Markham   DRUGS

Marine Compounds and Cancer: Updates 2020

(2020) Sergey A. Dyshlovoy et al.   Marine Drugs

Novel Auristatins with High Bystander and Cytotoxic Activities in Drug-Efflux Positive Tumor Models

(2020) Philip N. Moquist et al.   MOLECULAR CANCER THERAPEUTICS

SHR-A1403, a novel c-Met antibody-drug conjugate, exerts encouraging anti-tumor activity in c-Met-overexpressing models

(2019) Chang-yong Yang et al.   ACTA PHARMACOLOGICA SINICA

Antitumor activity of a 5T4 targeting antibody drug conjugate with a novel payload derived from MMAF via C-Lock linker

(2019) Baoying Shi et al.   Cancer Medicine

Discovery of a novel EGFR targeting antibody-drug conjugate, SHR-A1307, for the treatment of solid tumors resistant or refractory to anti-EGFR therapies

(2019) Kaijie He et al.   MOLECULAR CANCER THERAPEUTICS

The “Utility” of Highly Toxic Marine-Sourced Compounds

(2019) David J. Newman   Marine Drugs

SHR ‐A1403, a novel c‐mesenchymal‐epithelial transition factor (c‐Met) antibody‐drug conjugate, overcomes AZD 9291 resistance in non‐small cell lung cancer cells overexpressing c‐Met

(2019) Mengya Tong et al.   CANCER SCIENCE

First-in-Human Phase I Study of Aprutumab Ixadotin, a Fibroblast Growth Factor Receptor 2 Antibody–Drug Conjugate (BAY 1187982) in Patients with Advanced Cancer

(2019) Sung-Bae Kim et al.   Targeted Oncology

Belantamab mafodotin for relapsed or refractory multiple myeloma (DREAMM-2): a two-arm, randomised, open-label, phase 2 study

(2019) Sagar Lonial et al.   LANCET ONCOLOGY

Synthesis and evaluation of novel dolastatin 10 derivatives for versatile conjugations

(2018) Shinya Yokosaka et al.   BIOORGANIC & MEDICINAL CHEMISTRY

Metabolism of an Oxime-Linked Antibody Drug Conjugate, AGS62P1, and Characterization of Its Identified Metabolite

(2018) Josh T. Snyder et al.   MOLECULAR PHARMACEUTICS

Synthesis and Evaluation of Dolastatin 10 Analogues Containing Heteroatoms on the Amino Acid Side Chains

(2017) Julien Dugal-Tessier et al.   JOURNAL OF NATURAL PRODUCTS

Current Status of Marine-Derived Compounds as Warheads in Anti-Tumor Drug Candidates

(2017) David Newman et al.   Marine Drugs

Preclinical Antitumor Efficacy of BAY 1129980—a Novel Auristatin-Based Anti-C4.4A (LYPD3) Antibody–Drug Conjugate for the Treatment of Non–Small Cell Lung Cancer

(2017) Jörg Willuda et al.   MOLECULAR CANCER THERAPEUTICS

A practical approach to asymmetric synthesis of dolastatin 10

(2017) Wen Zhou et al.   ORGANIC & BIOMOLECULAR CHEMISTRY

Synthesis and biological activity evaluation of dolastatin 10 analogues with N-terminal modifications

(2017) Xin Wang et al.   TETRAHEDRON

Preclinical Efficacy of the Auristatin-Based Antibody–Drug Conjugate BAY 1187982 for the Treatment of FGFR2-Positive Solid Tumors

(2016) Anette Sommer et al.   CANCER RESEARCH

Recent Advances in the Development of New Auristatins: Structural Modifications and Application in Antibody Drug Conjugates

(2015) Andreas Maderna et al.   MOLECULAR PHARMACEUTICS

Discovery of Cytotoxic Dolastatin 10 Analogues with N-Terminal Modifications

(2014) Andreas Maderna et al.   JOURNAL OF MEDICINAL CHEMISTRY

Marine-Sourced Anti-Cancer and Cancer Pain Control Agents in Clinical and Late Preclinical Development

(2014) David Newman et al.   Marine Drugs

A Synthetic Dolastatin 10 Analogue Suppresses Microtubule Dynamics, Inhibits Cell Proliferation, and Induces Apoptotic Cell Death

(2013) Praveen Kumar Gajula et al.   JOURNAL OF MEDICINAL CHEMISTRY

The discovery and development of brentuximab vedotin for use in relapsed Hodgkin lymphoma and systemic anaplastic large cell lymphoma

(2012) Peter D Senter et al.   NATURE BIOTECHNOLOGY

Antineoplastic Agents. 592. Highly Effective Cancer Cell Growth Inhibitory Structural Modifications of Dolastatin 10

(2011) George R. Pettit et al.   JOURNAL OF NATURAL PRODUCTS

A Straightforward Approach to Protected (S)-Dolaphenine (Doe), the Unusual Amino Acid Component of Dolastatin 10

(2011) Uli Kazmaier et al.   SYNTHESIS-STUTTGART

Novel Peptide Linkers for Highly Potent Antibody−Auristatin Conjugate

(2008) Svetlana O. Doronina et al.   BIOCONJUGATE CHEMISTRY

Phase I study of TZT-1027, a novel synthetic dolastatin 10 derivative, for the treatment of patients with non-small cell lung cancer

(2008) J. Horti et al.   CANCER CHEMOTHERAPY AND PHARMACOLOGY

Phase I study of TZT-1027, a novel synthetic dolastatin 10 derivative and inhibitor of tubulin polymerization, given weekly to advanced solid tumor patients for 3 weeks

(2008) Nobuyuki Yamamoto et al.   CANCER SCIENCE

Structural insight into the inhibition of tubulin by vinca domain peptide ligands

(2008) Anthony Cormier et al.   EMBO REPORTS

Stereoselective synthesis of the dolastatin units by organotrifluoroborates additions to α-amino aldehydes

(2007) Rodrigo Cella et al.   TETRAHEDRON LETTERS