Top 5 Companies Developing Peptide Drug Conjugate

Published: December 2023

These peptide drug conjugate developers are all set to revolutionize the field of next generation drug conjugates with their efforts to develop targeted therapeutic candidates for various disease indications. We analyzed over 30 companies that are engaged in the development of more than 200 next generation drug conjugates, across different stages of development. In this article, we unveil 5 leading companies that are engaged in developing peptide drug conjugate and their capabilities in this industry.

Over the last decade, the standard cost of medical care for rare disease indications has increased exponentially. Specifically, in the US, close to USD 1 trillion was spent for medical care for rare diseases in 2020. Further, the average cost incurred by a patient suffering from a rare disease condition was USD 60,248 in 2020, which if taken into account is twice the average cost incurred by any general patient. The incremental rise in medicare cost, coupled with the rising burden of rare disease indications globally, prompted the stakeholders to look for alternatives to the conventional therapies, and next generation drug conjugates have emerged as a promising treatment option.

Similar to antibody drug conjugates (ADCs), the next generation drug conjugates utilize a targeting ligand, a linker and a payload for the targeted delivery. However, unlike the ADCs which uses antibody as the targeting ligand, the next generation drug conjugates utilize various non-antibody-based targeting ligands such as peptide, amino sugar, lipid, and small molecule as their targeting ligand. On the other hand, in lieu of drug as its payload / warheads, these next generation drug conjugates incorporate si-RNAs, oligonucleotide, antisense oligonucleotide, and radionuclide.

Given the various combination available with the targeting ligand and the payload, various types of next generation drug conjugates, such as peptide drug conjugate, peptide oligonucleotide conjugate, peptide radionuclide conjugate, small molecule-drug conjugate (SMDC), ligand conjugated anti sense medicine (LICA), ligand medicated RNAi conjugate, peptide conjugated phosphorodiamidate morpholino oligomers (PPMO) have emerged in this industry.

The biological properties of peptides, such as improved cell metabolism, prevention of cell degeneration and cell repair, result in its widespread usage as an important moiety in targeted next-generation treatment option for various diseases, including oncological disorders, metabolic disorders, infectious diseases and immunological disorders. Moreover, peptide drug conjugates confer various advantages over ADCs, such as small size, strong tissue penetration, high selectivity, enhanced cellular permeability and easy industrial synthesis. This could potentially result in improved target specificity and intracellular uptake of the drug in the patients. Currently, more than 30 developers are currently developing next generation drug conjugates (including peptide drug conjugates) across various stages of development.
Roots Analysis has conducted an exhaustive study of the Next Generation Drug Conjugates Market featuring the current market landscape and future opportunity associated with next generation drug conjugates (GalNac Conjugates, peptide drug conjugates, peptide oligonucleotide conjugates, rnai conjugates, peptide receptors radionuclide therapies, SMDCs and other conjugates), over a span of 12 years.

Table of Contents: Top Companies Developing Peptide Drug Conjugates

In the table below, we have listed (in decreasing order of number of peptide drug conjugates being developed), the top 5 peptide drug conjugate developers.

Table: List of Top 5 Companies Ddeveloping Peptide Drug Conjugates

Company    Year of Establishment                    Headquarters    Number of Employees                             
Coherent Biopharma 2016 Suzhou, China 51-200
Bicycle Therapeutics 2009 Cambridge, England 201-500
Cybrexa Therapeutics 2017 New Haven, Connecticut 11-50
Mainline Biosciences 2014 Malvern, Pennsylvania 2-10
Angiochem 2003 Westmount, Quebec 11-50

Source: Roots Analysis

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Discover the Details on Top 5 Companies Developing Peptide Drug Conjugates

This article highlights the top companies that are engaged in the development of peptide drug conjugates to watch out in this industry. These companies were chosen based on the number of peptide drug conjugates in their drug pipeline (more than two pipeline candidates). It is essential to note that the selection of top players can differ substantially according to the defined criteria.

1. Coherent Biopharma is Committed towards the Development of Multi-Targeted Ligand Conjugated Drugs

Coherent Biopharma was founded in 2016 and is headquartered in Suzhou, China. The company aims to accelerate the progress of its therapeutic candidates, from laboratory to clinic, based on its Bi-Engaging ligand-mediated Selective Targeting (BESTTM) platform. The company claims to be working in different modalities, including bi-targeting ligand drug conjugates (Bi-XDC) and tumor marker diagnostic reagents. In February 2023, the company announced the expansion of its capability through the establishment of R&D center and a production facility at Hefei National High-tech Industry Development Zone.

Coherent Biopharma is engaged in the development of following peptide drug conjugates:

  • CBP-1008 (currently in Phase II; for Breast and Ovarian Cancer)
  • CBP-1019 (currently in Phase I / II; for Pancreatic, Lung and Colorectal Cancer)
  • CBP-1018 (currently in Phase I; for Prostate and Lung Cancer)
  • CBP-1029 (currently in Preclinical; for Solid Tumors)
  • CBP-1039 (currently in Preclinical; for Solid Tumors)

Recent Developments:

In June 2023, Coherent Biopharma presented positive clinical data from phase I study of CBP-1008 at the 2023 American Society of Clinical Oncology (ASCO) annual meeting.1 In May 2023, the company raised USD 100 million through Venture funding (Series B and B+) in order to support the development of Bi-XDC drugs.

Key Strengths:

The company’s clinical pipeline, consist of first-in-class bioconjugates that utilize biomarker assays for screening the patients and are based on the receptor mediated internalization and cytotoxicity. With the initiation of phase II clinical trials of CBP1008, the company has been able to demonstrate the capability of its BEST platform for targeting multiple tumor targeted drugs.

2. Through Collaborations with Various Strategic Partners, Bicycle Therapeutics Aims to Develop Novel Precision-Guided Therapeutic Modalities

Bicycle Therapeutics is a clinical stage company based in UK that is engaged in the development of a highly selective and stabilized bi-cyclic looped structure of peptides (referred to as Bicycles). The company claims to develop various types of bicycles, including monomeric bicycles, bicyclic toxin conjugates (BTC) and multi-specific bicycles, for the treatment of various diseases, such as infectious diseases, oncological disorders, immune-oncological disorders, neuromuscular disorders and ophthalmological disorders. Over time, the company has developed an extensive intellectual portfolio pertaining to bicycle peptide (Bicycle®) technology.

Bicycle Therapeutics is engaged in the development of following peptide drug conjugates:

  • BT1718 (currently in Phase II; for Advanced Solid Tumors)
  • BT5528 (currently in Phase I / II; for Ovarian, Urothelial, Lung, Head and Neck, Upper Gastrointestinal, and Triple Negative Breast Cancer)
  • BT5528 in combination with nivolumab (currently in Phase I / II; for Ovarian, Urothelial, Lung, Head and Neck, Upper Gastrointestinal, and Triple Negative Breast Cancer)
  • BT8009 (currently in Phase I / II; for Multiple Solid Tumors)
  • BT8009 in combination with pembrolizumab (currently in Phase I / II; for Multiple Solid Tumors)

Recent Developments:

In October 2023, the FDA selected BT8009 for the inaugural cohort of new Chemistry, Manufacturing and Controls (CMC) Development and Readiness Pilot (CDRP) program in order to accelerate its commercial manufacturing readiness.2 Earlier, in July 2023, the company raised USD 215.1 million through secondary offering.

Key Strengths:

Bicyclic Therapeutics is looking to expedite the clinical development and regulatory pathway for BT8009 for the treatment of urothelial cancer. The company announced its plan to conduct Phase II / III registration trial in early 2024. Currently, the company is extensively engaged in the development of third generation BTC and Natural Killer (NK) cell engagers.

3. Combinatorial Therapy Approach Adopted by Cybrexa Therapeutics aims to Revolutionize the Standard-of-Care Treatment Option for Cancer Patients.

Cybrexa Therapeutics is a clinical-stage company focused on the development of novel antigen-independent tumor-targeting peptide drug conjugates. The company leverages its alphalex™ technology platform for the targeted, intracellular delivery of potent anti-cancer therapeutics in the patient’s body. This technology claims to have several advantages over the other conventional platforms, such as broader applicability to diverse types of tumors, reduced systemic exposure and selective differentiation of tumor and healthy cells. The formation of alpha-helical structure of the peptide (pHLIP) in low pH tumor microenvironment leads to selective targeting of the drug in the patients.

Cybrexa Therapeutics is engaged in the development of following peptide drug conjugates:

  • alphalex™-exatecan1 (CBX-12) (currently in Phase II; for Multiple Solid Tumors)
  • alphalex™-MMAE (CBX-15) (currently in Preclinical; for Multiple Solid Tumors)
  • alphalex™-DM4 (CBX-13) (currently in Preclinical; for Multiple Solid Tumors)
  • alphalex™-multi-targeted DR inhibitor (CBX-14) (currently in Discovery; for Multiple Solid Tumors)
    Note 1: It is important to note that the rights to CBX-12 were acquired by Exelixis in November 2022

Recent Developments:

In October 2023, the company presented the preclinical data findings of CBX-15 at 35th AACR-NCI-EORTC (ANE) symposium. Earlier, in May 2023, the company presented data of CBX-12 from Phase I clinical study at 2023 ASCO annual meeting. The data showed that as a single agent, CBX-12 demonstrated multiple objective responses and manageable side-effects in the patients.

Key Strengths:

With a focus on toxin conjugates and DNA damage repair (DDR) inhibition, Cybrexa Therapeutics is committed to develop a robust portfolio of therapeutics targeting solid tumors. The company claims to be in discussions with various stakeholders in the industry in order to license its technology and expand its pipeline candidates.

4. Extensive Research Capabilities at Mainland Sciences Thrives to Develop Advanced Peptide-based Therapeutics

Mainline Sciences is a US-based company that is engaged in the development of various peptide-based drugs the treatment of patients suffering from cancer, obesity, pain and fibrosis. The company has developed its own peptide drug conjugate and bispecific peptide drug development platform, which is based on rational designing and drug discovery. The company claims to have requisite capabilities for drug designing, screening, evaluation, discovery  and development.

Mainline Biosciences is engaged in the development of following peptide drug conjugates:

  • MB1707 (currently in Phase I; for Breast, Pancreatic and Lung Cancer)
  • MB1801 (currently in Preclinical; for Brain Metastasis Tumors)
  • MB2001 (currently in Preclinical; for Solid Tumors) 
  • MB2101 (currently in Preclinical; for Solid Tumors)

Recent Developments:

In December 2022, the Phase I study of MB1707 (a potent CXC chemokine receptor 4 antagonist) was initiated in order to evaluate its pharmacokinetics and safety profile in patients suffering from cancer. As per the company’s website, this therapeutic modality, in combination with irradiation, antiangiogenic agent or immunotherapeutic checkpoint antagonist, can result in a synergistic effect for cancer treatment.

Key Strengths:

With the development of therapies that based on cancer-specific surface target mediated cytotoxicity, Mainline Biosciences aims to become a leader in the field of innovative peptide drugs. The company claims to be consistently working towards clinical development of its candidates.

5. Angiochem is Focused on Developing Breakthrough Brain-Targeting Therapies by Harnessing Body’s Active Transport System

Angiochem is a biotechnology company focused on the development of peptide drug conjugates for the treatment of neurological disease. The firm claims that the products of its proprietary Engineered Peptide Compound technology platform consist of a specific amino acid sequence (Angiopeps) that targets the lipoprotein receptor-related protein (LRP-1) receptor. The company’s proprietary technology platform claims to leverage the LRP-1 mediated pathway in order to cross the blood brain barrier, and maintain the drug efficacy and activity at the same time. It is worth mentioning that the company states to have developed a proprietary library of over 100 peptide structures (8-34 amino acids long) that are being used to develop the various drug candidates.

Angiochem is engaged in the development of following peptide drug conjugates:

  • ANG-1005 (currently in Phase III; for Leptomeningeal Carcinomatosis caused by Breast Cancer Brain Metastases (BCBMLC))
  • ANG-1007 (currently in Preclinical; for BCBMLC)
  • ANG-2002 (currently in Preclinical; for Acute, Inflammatory, Post-Operative, Cancer and Neuropathic Pain)

Recent Developments:

In December 2023, the open-label Phase II study was initiated in order to observe the prolonged survival effect of ANG-1005 (as compared to physician’s best choice control) in the patients suffering from BCBMLC. As per the company’s website, its EpiC technology has been validated for drug efficacy and safety amongst 200+ patients across four clinical trials and in various preclinical studies.

Key Strengths:

The company’s technology has been designed to support the development of small molecules and biologics for the treatment of various serious diseases, including neurological disorders, oncological disorders, metabolic disorders and pain. This technology will prove helpful for the company to maintain the activity of its pipeline products.

Are you curious to gain more insights on the in-depth analysis of the various firms / organizations that are engaged in next generation drug conjugates market?

The above presentation features five peptide drug conjugate developers selected from a pool of over 30 next generation drug developers that we have compiled. If you are interested, you can download the Sample Report on “Next Generation Drug Conjugates Market” by Roots Analysis. For personalized assistance in identifying the most relevant solutions based on your specific criteria, please don't hesitate to reach out to us at


About Author


Prachi holds an M.Tech. degree in Biotechnology from Indian Institute of Technology, Guwahati and B.E. degree in Biotechnology from Panjab University. Upon completing her postgraduate studies, she embarked on her research career by securing the position of Senior Research Fellow at PGIMER, Chandigarh. In her more than two years of scientific career, she honed her skills in the field of cell and molecular biology, pathology and organic chemistry. Prachi has over two years of remarkable experience in the business research and consulting domain. She is equipped with the distinctive skill set to thrive and contribute immensely to the development of syndicate reports and assignments pertaining to the pharmaceutical and biotechnology industry. She has persistently sought to present impactful, critical insights to the clients through several drug-based, product-based, technology-based and service-based research reports.


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