HER2 antagonists(Receptor tyrosine-protein kinase erbB-2 antagonists), Tubulin inhibitors, ADCC(Antibody-dependent cell-mediated cytotoxicity (ADCC) effects)

Therapeutic Areas

NeoplasmsDigestive System Disorders

Active Indication

Stomach Cancer

Inactive Indication

Metastatic human epidermal growth factor 2 positive carcinoma of breast

Originator Organization

Alteogen, Inc.

Active Organization

Shenyang Sunshine Pharmaceuticals Co., Ltd.

Inactive Organization

Alteogen, Inc.

License Organization

Shenyang Sunshine Pharmaceuticals Co., Ltd.

Alteogen, Inc.

Gachon University Gil Medical Center

Drug Highest PhasePhase 1

First Approval Date-

Regulation-

Structure/Sequence

Molecular FormulaC39H67N5O7

InChIKeyDASWEROEPLKSEI-UIJRFTGLSA-N

CAS Registry474645-27-7

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Sequence Code 18481L

The sequence is quoted from: *****

Sequence Code 44772H

The sequence is quoted from: *****

Clinical Trials associated with ALT-P7

NCT03281824

/ CompletedPhase 1

Open-Label, Dose Increase and Phase I Study of ALT-P7 to Determine Safety, Tolerability, Pharmacokinetics for HER2 Positive Metastatic Breast Cancer Patients Who Have Progressed on Previous Trastuzumab-Based Therapy

This open-label study assessed the safety, tolerability and pharmacokinetics of ALT-P7(HM2-Drug Conjugate) in patients with HER2-positive metastatic breast cancer who have progressed on previous Trastuzumab-based therapy. Patients received ALT-P7(0.3 mg/kg
5.4 mg/kg, 7 groups) intravenously on Day 1 of each 3-week cycle.

Start Date11 Jan 2018

Sponsor / Collaborator

Alteogen, Inc.

100 Clinical Results associated with ALT-P7

100 Translational Medicine associated with ALT-P7

100 Patents (Medical) associated with ALT-P7

566

Literatures (Medical) associated with ALT-P7

01 Apr 2025·Bioorganic & Medicinal Chemistry

Fine-tuning phenoxy silyl scaffolds for the development of glutathione-responsive prodrugs and antibody–drug conjugates

Article

Author: Jiang, Yuecheng ; Wang, Huihui ; Huangfu, Shangwei ; Jiang, Biao ; Chen, Hongli ; Wei, Ding ; Qi, Cheng ; Yu, Xianqiang

Silyl ether is particularly attractive for application in drug development for its easy preparation, non-toxicity and remarkable biocompatibility. Earlier studies relied on the use of intracellular acidic conditions to induce the cleavage of alkoxy silyl ethers. However, acidic conditions are not suitable to trigger the release of phenoxy silyl ethers, since they are more stable under acidic conditions compared with neutral conditions. We explored the vulnerability of the phenoxy silyl ether towards biological nucleophilic reagents and found that glutathione (GSH) could effectively and selectively induce the cleavage of phenoxy silyl ether. We also demonstrated that the rate of cleavage was controllable by adjusting the substituents on the phenyl ring. Phenoxy silyl ether-based prodrugs and antibody-drug conjugates (ADCs) were designed and synthesized, which could be effectively activated in cells with high GSH levels and there was an obvious therapeutic window between cells with different GSH levels.

19 Feb 2025·Bioconjugate Chemistry

A Unique Prodrug Targeting the Prostate-Specific Membrane Antigen for the Delivery of Monomethyl Auristatin E

Article

Author: Berkman, Clifford E. ; Savoy, Emily A. ; Bomba, Hunter N. ; Fulton, Melody D. ; Langton-Webster, Beatrice

Monomethyl auristatin E (MMAE) is a promising treatment option for patients diagnosed with prostate cancer (PCa); however, toxicities prevent MMAE from being administered as free drug. No MMAE-based treatment is currently marketed for PCa. Herein, we describe a small-molecule-drug conjugate, CTT2274, for the selective delivery of MMAE. CTT2274 is composed of a prostate-specific membrane antigen (PSMA)-binding scaffold, a biphenyl motif, a pH-sensitive phosphoramidate linker, and MMAE payload. We demonstrate that CTT2274 shows selective binding to PSMA, which is overexpressed on PCa cells, and induces tumor cell death in vitro. In a patient-derived xenograft tumor model of PCa in mice, we show that weekly intravenous dosing of CTT2274 at 3.6 mg/kg for six weeks is superior to treatment with free MMAE at equivalent doses. Mice treated with CTT2274 experienced prolonged tumor suppression and significantly greater overall survival than mice treated with PBS. Additionally, the safety of CTT2274 compared to an equivalent dose of MMAE was assessed in healthy, non-tumor-bearing mice. Our results demonstrate that CTT2274 therapy is as efficacious as MMAE, results in superior overall survival, and has a more favorable safety profile. Together, these data indicate that CTT2274 is a candidate for clinical translation for the treatment of PCa.

18 Feb 2025·ACS Nano

Nanobody-Mediated Cellular Uptake Maximizes the Potency of Polylysine Dendrimers While Preserving Solid Tumor Penetration

Article

Author: Feeney, Orlagh M. ; Johnston, Angus P.R. ; Humphries, James ; Noi, Leo ; Owen, David J. ; Porter, Christopher J.H. ; Cullinane, Carleen ; Fletcher, Nicholas L. ; Yuen, Daniel ; Houston, Zachary H ; Thurecht, Kristofer J. ; Reitano, Pauline ; Hufton, Richard ; McLeod, Victoria M. ; Shengule, Sudhir ; Tsegay, Sammi

Dendrimers are branched macromolecular structures that are useful nanocarriers for small-molecule drugs, such as cancer therapeutics. Their small size permits penetration into solid tumors, coupled with functionalization with a low-fouling PEG coating that minimizes transient cellular interactions and enhances plasma circulation time. While PEGylated dendrimers show significant promise as anticancer therapeutics, there is potential to increase tumor cell specificity and drive uptake of drugs into cells by conjugating cell-targeting ligands onto the dendrimers. To achieve this, we used an expanded genetic code and bio-orthogonal click chemistry to functionalize monomethyl auristatin E (MMAE)-loaded PEGylated dendrimers with a single tumor cell-targeting nanobody per dendrimer. The uniform addition of a single nanobody ligand facilitated greater intracellular uptake of the drug payload into HER2-positive target cells, while preserving the desirable circulatory characteristics of dendrimers. While the nanobody-dendrimer conjugates show similar levels of tumor infiltration over 24 h compared to unmodified dendrimers, the targeted dendrimers had significantly greater inhibition of tumor growth and long-term retention in the tumors. Our results highlight that biodistribution studies alone are poor predictors of therapeutic performance. The controlled conjugation strategy presented here preserves the size advantage and tissue penetration of dendrimers while maximizing targeted cellular uptake and potency in difficult-to-access solid tumor tissue.

100 Deals associated with ALT-P7

R&D Status

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Stomach Cancer	Phase 1	China	Shenyang Sunshine Pharmaceuticals Co., Ltd.	-
Metastatic human epidermal growth factor 2 positive carcinoma of breast	Preclinical	South Korea	Alteogen, Inc.	11 Jan 2018

Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT03281824 (ASCO2020)	Phase 1	Advanced HER2-Positive Breast Carcinoma	27	ALT-P7	yhyxprkkao(lwvscciajj) = alopecia occurred in 6 patients kcwegliheo (ahfcveohmt ) View more	Positive	25 May 2020

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