Development Pipeline | Investor Relations | CHUGAI PHARMACEUTICAL CO., LTD.

Chugai’s development pipeline is categorized to Oncology, Immunology, Neuroscience, Hematology, Ophthalmology, and Other diseases. In addition, we disclose “Response to Requests from the MHLW Review Committee on Unapproved Drugs and Indications with High Medical Needs.”
View the status of our current development pipeline as of July 25, 2024 in a PDF format.

Basic Information on Development Pipeline^*
*Exclude products that have already obtained regulatory approval

Oncology

In-house / Roche / Others	Modality/ Administration	Generic name, Development Code, Mode of Action	Indication	Basic Information
In-house	mid-size molecule Oral	LUNA18 RAS inhibitor	Solid tumors	LUNA18, the first project in mid-size molecule drug project, is an orally administrable cyclic peptide molecule created by Chugai’s unique mid-size molecule drug discovery platforms. It inhibits protein-protein interaction between RAS and GEF to retain RAS in an inactive state. LUNA18 exhibits growth inhibitory activity against tumor cells with various RAS alterations (mutations or amplifications) and can be expected to have anti-tumor effects against cancers with RAS alterations where there are no therapeutic drugs yet.
In-house	antibody IV	codrituzumab/GC33 Anti-Glypican-3 humanized monoclonal antibody	HCC	GC33, a humanized monoclonal antibody created by Chugai, targets glypican-3 (GPC3), which is specifically expressed in hepatocellular carcinoma.
In-house	antibody IV	ERY974 Anti-Glypican-3/CD3 bispecific antibody	Solid tumors	ERY974 is the first T-cell redirecting antibody (TRAB^™) developed by Chugai. TRAB^™ is a bispecific antibody that creates a short bridge between CD3 on T cells and tumor antigen on tumor cells to activate T cells in a tumor antigen-dependent manner, and is expected to demonstrate strong cytotoxicity against tumor cells.
In-house	antibody IV	STA551 Anti-CD137 agonistic Switch antibody	Solid tumors	STA551, a “Switch Antibody^™,” is the first application of Switch Antibody^™ technology, which was developed by Chugai. Switch antibodies bind to the target antigen only where there is a high concentration of a certain “switch” molecule, which is concentrated specifically at the diseased site. STA551 binds to CD137 and activates T cells in the presence of the switch molecule ATP, but not in the absence of ATP. It therefore promises to act selectively on tumor tissue.
In-house (licensed out to Roche)	antibody IV	SOF10/RG6440 Anti-latent TGF-β1 monoclonal antibody	Solid tumors	SOF10, a monoclonal antibody created by Chugai, binds to latent TGF-β1 and inhibit the activation. By changing the immunosuppressive tumor microenvironment, such as developing fibrosis of tumor tissue, an anti-tumor effect is expected against cancers where anti-cancer drugs do not respond.
In-house (licensed out to Roche)	antibody IV	ALPS12/RG6524 Anti-DLL3/CD3/CD137 trispecific antibody	Solid tumors	ALPS12 is the first next-generation T-cell redirecting antibody applying Chugai’s proprietary Dual-Ig^® technology. T-cell redirecting antibody (TRAB^™) is designed to guide T cells to the target cancer cells by activating and engaging T cells through its binding to CD3 on T cells. One of its challenges, however, is that it has limited antitumor killing ability against poorly T-cell infiltrated tumors. Dual-Ig^® is a novel technology providing antibodies with the ability to induce CD137 signalling, a co-stimulating molecule, in addition to CD3 signalling. This property potentially results in more potent antitumor effect against poorly T-cell infiltrated tumors than conventional T-cell engagers.
In-house	antibody IV	SAIL66 Anti-CLDN6/CD3/CD137 trispecific antibody	CLDN6 positive solid tumors	SAIL66 is the next-generation T-cell redirecting antibody applying Chugai’s proprietary Dual-Ig^® technology. T-cell redirecting antibody (TRAB^™) is designed to guide T cells to the target cancer cells by activating and engaging T cells through its binding to CD3 on T cells. One of its challenges, however, is that it has limited antitumor killing ability against poorly T-cell infiltrated tumors. Dual-Ig^® is a novel technology providing antibodies with the ability to induce CD137 signalling, a co-stimulating molecule, in addition to CD3 signalling. This property potentially results in more potent antitumor effect against poorly T-cell infiltrated tumors than conventional T-cell engagers.
In-house	antibody IV	ROSE12 ―	Solid tumors	ROSE12 is an antibody drug developed in-house by Chugai. It is applied to Switch Antibody^™ technology and is expected to work selectively on tumor tissue.
In-house	small molecule Oral	SPYK04 ―	Solid tumors	SPYK04 is a small molecule drug developed in-house by Chugai.
In-house (licensed out to 3^rd party)	small molecule Oral	avutometinib/VS-6766 RAF/MEK clamp	Recurrent LGSOC NSCLC mPDAC	Avutometinib is an oral RAF/MEK clamp developed in-house by Chugai. In January 2020, Chugai granted Verastem Oncology an exclusive worldwide license to manufacture, develop and commercialize CKI27.
Roche	antibody IV	tiragolumab/RG6058 Anti-TIGIT human monoclonal antibody	NSCLC NSCLC (stage III) Esophageal cancer HCC	RG6058 is an anti-TIGIT monoclonal antibody in-licensed from Roche. TIGIT is an immune checkpoint expressed on the surface of NK cells and T cells that binds to poliovirus receptors (PVR) expressed on tumor cell surfaces. This binding is thought to allow the cancer cells to evade attack by immune cells. RG6058 restores and maintains the immune response of NK cells and T cells by blocking the binding of TIGIT to PVR, and is thus expected to demonstrate efficacy against cancer cells.
Roche	antibody IV/SC	mosunetuzumab/RG7828 Anti-CD20/CD3 bispecific antibody	Follicular lymphoma relapsed or refractory aggressive B-cell non-Hodgkin lymphoma	RG7828 is a bispecific antibody in-licensed from Roche. It is expected to activate T cells and attack tumor cells by crosslinking CD3 on T cells to CD20 on B cells.
Roche	antibody IV	glofitamab/RG6026 Anti-CD20/CD3 bispecific antibody	Previously untreated large B-cell lymphoma	RG6026 is a bispecific antibody in-licensed from Roche. By cross-linking CD3 on T cells with CD20 on B cells, it is expected to cause T-cell activation and proliferation and attack on the target B cells through cytokine release, resulting in antitumor effect.
Roche	antibody IV	runimotamab/RG6194 Anti-HER2/CD3 bispecific antibody	Solid tumors	RG6194, an anti-HER2/CD3 bispecific antibody in-licensed from Roche, is expected to act against HER2-expressing cancer cells by inducing and activating T cells.
Roche	antibody IV	cevostamab/RG6160 Anti-FcRH5/CD3 bispecific antibody	Relapsed or refractory multiple myeloma	RG6160 is a humanized bispecific monoclonal antibody in-licensed from Roche against FcRH5/CD3 that binds to FcRH5 on myeloma cells and CD3 on T cells, and it is expected to activate cytotoxic T cell-mediated immunity and kill myeloma cells.
Roche	small molecule Oral	giredestrant/RG6171 Selective Estrogen Receptor Degrader (SERD)	Breast cancer Breast cancer (adjuvant)	RG6171 is a selective estrogen receptor degrader (SERD) in-licensed from Roche. It is expected to exert a stronger anti-estrogen effect by promoting the degradation of ER as well as competitively inhibiting estrogen receptor binding.
Roche	small molecule Oral	cobimetinib/RG7421 MEK inhibitor	Solid tumors	RG7421 is an MEK inhibitor in-licensed from Roche.
Roche	small molecule Oral	divarasib/RG6330 KRAS G12C inhibitor	Solid tumors	RG6330 is designed as an orally available small molecule, and preclinical models showed potent and selective inhibition of the KRAS G12C protein. The combination with RG6433 will be expected synergistic anti-tumor activity.
Roche	antibody IV	tobemstomig/RG6139 Anti-PD-1/LAG-3 bispecific antibody	Solid tumors	RG6139 is a bispecific antibody binding to PD-1 and LAG-3, which reinvigorates T cells by blocking two co-inhibitory checkpoint receptors. It preferentially targets tumor-reactive tumor infiltrating lymphocytes (TILs), and avoids immunosuppressive effects by preferential binding to effector T cells vs regulatory T cells (Tregs).

Immunology

In-house / Roche / Others	Modality/ Administration	Generic name, Development Code, Mode of Action	Indication	Basic Information
In-house	antibody SC	DONQ52 Anti-HLA-DQ2.5/gluten peptides multispecific antibody	Celiac disease	DONQ52 is a multispecific antibody against complex of HLADQ2.5/gluten peptides. DONQ52 directly inhibits gluten dependent T cell activation by neutralizing interaction of T cell receptor (TCR) and complex of HLA-DQ2.5/gluten peptides. DONQ52 covers >25 gluten derived peptides including all immunodominant gluten peptides for celiac disease. Gluten-specific blockade enables long-acting (subcutaneous injection) and high safety profile.
In-house	antibody ―	RAY121 Anti-complement C1s recycling antibody	Autoimmune disease	RAY121 is a therapeutic antibody that applies the recycling antibody^® technology created by Chugai.
Roche	nucleic acid SC	RG6299 Antisense oligonucleotide targeting complement factor B mRNA	IgA nephropathy	RG6299 is an ASO targeting complement factor B (CFB) mRNA. CFB is one of the molecules involved in activation of the alternative complement pathway that contributes to IgA nephropathy. After RG6299 specifically binds to CFB mRNA, synthesis of CFB is inhibited, which is expected to inhibit progression of IgA nephropathy.

Neuroscience

In-house / Roche / Others	Modality/ Administration	Generic name, Development Code, Mode of Action	Indication	Basic Information
In-house (licensed out to Roche)	antibody SC	GYM329/RG6237 Anti-latent myostatin sweeping antibody	Neuromuscular disease Spinal muscular atrophy Facioscapulohumeral muscular dystrophy (FSHD) Obesity	GYM329, created by Chugai, is a next-generation antibody that applies Chugai’s proprietary antibody engineering technologies, including its recycling antibody^® and sweeping antibody^® technologies. Latent myostatin is an inactive form that is mainly secreted from muscle cells, and is activated by BMP-1 and other protein degrading enzymes. Activated myostatin inhibits muscle growth and hypertrophy, and by inhibiting myostatin action, GYM329 is expected to improve the various conditions associated with muscle atrophy and loss of muscular strength.
Roche	antibody IV	prasinezumab/RG7935 Anti-α-synuclein monoclonal antibody	Parkinson’s disease	RG7935 is a monoclonal antibody that targets α-synuclein. It slows the expansion of nerve cell death by inhibiting the cell-to-cell propagation of aggregated forms of neurotoxic α-synuclein, and is expected to reduce and delay progression of the disease.
Roche	antibody IV	trontinemab/RG6102 Anti-amyloid beta/TfR1 fusion protein	Alzheimer’s disease	RG6102 is an anti-amyloid beta/TfR1 fusion protein with a novel transferrin receptor (TfR1) binding Ab moiety to achieve efficient transport over the BBB and target Aβ engagement in the brain. It is potential for superior Aβ clearance in brain to delay progression of Alzheimer’s disease.
Roche	nucleic acid IV	tominersen/RG6042 Antisense oligonucleotide targeting HTT mRNA	Huntington’s disease	RG6042 is an ASO targeting human HTT mRNA, which is believed to be the cause of Huntington’s disease. It has the potential to delay or slow disease progression in people with Huntington’s disease by binding specifically to HTT mRNA, after which synthesis of the HTT protein is inhibited.
Roche	gene therapy IV	RG6356/SRP-9001 Micro-dystrophin gene therapy	Duchenne muscular dystrophy (DMD)	RG6356 is an investigational gene transfer therapy developed for targeted muscle expression of micro-dystrophin, a shortened, functional dystrophin protein, that addresses the genetic cause of DMD. Sarepta manages the global study including Japan.

Hematology

In-house / Roche / Others	Modality/ Administration	Generic name, Development Code, Mode of Action	Indication	Basic Information
In-house (licensed out to Roche)	antibody SC	NXT007/ RG6512 Anti-coagulation factor IXa/X bispecific antibody	Hemophilia A	NXT007, created by Chugai, is a bispecific antibody that stimulates blood coagulation using the same mode of action as Hemlibra. It is applied with Chugai’s antibody engineering technologies FAST-Ig^™, which enhances large-scale production of the bispecific antibody and ACT-Fc^®, which is expected to improve antibody pharmacokinetics. NXT007 is expected to achieve the levels of hemostasis found in healthy adults and children, and is being developed to improve convenience, including the administration device.

Ophthalmology

In-house / Roche / Others	Modality/ Administration	Generic name, Development Code, Mode of Action	Indication	Basic Information
Roche	antibody injection via implant	ranibizumab (Port Delivery System)/ RG6321	Neovascular Age-related macular degeneration (nAMD) Diabetic macular edema	“RG6321” is Port Delivery System with ranibizumab. Ranibizumab is a Fab fragment of a recombinant humanized monoclonal antibody against vascular endothelial growth factor A (VEGF-A), and is already sold and supplied worldwide as Lucentis^® for intravitreal administration. This product is expected to maintain visual acuity without frequent dosing by the long-term and sustained release of ranibizumab from ocular implant with the highest formulation concentration.
Roche	antibody intravitreal injection	vamikibart/RG6179 Anti-IL-6 monoclonal antibody	Noninfectious uveitic macular edema	RG6179 is an anti-IL-6 antibody that is administrated with IVT injection should inhibit IL-6 signaling specifically, and expected to reduce intraocular inflammation and vascular hyperfiltration improve macular edema and visual acuity with fewer progression of cataract and lower risk of increased intraocular pressure compared to steroids. RG6179 is engineered on Fc region to increase its systemic clearance and is expected that risk of systemic side-effects induction should be decreased.

Other diseases

In-house / Roche / Others	Modality/ Administration	Generic name, Development Code, Mode of Action	Indication	Basic Information
In-house	antibody SC	AMY109 Anti-IL-8 recycling antibody	Endometriosis	AMY109 is the third therapeutic antibody to apply the recycling antibody^® technology created by Chugai. Its approach differs from hormone therapy, which is the standard treatment for endometriosis, and its anti-inflammatory action is expected to provide new value to patients.
In-house (licensed out to 3^rd party)	antibody SC	nemolizumab Anti-IL-31 receptor A humanized monoclonal antibody	Atopic dermatitis Prurigo nodularis Chronic kidney disease associated pruritus	Nemolizumab is an anti-IL-31 receptor A humanized monoclonal antibody originating from Chugai. The drug is expected to improve itching and skin inflammation in atopic dermatitis by blocking IL-31, a proinflammatory cytokine, from binding to its receptor. In July 2016, Chugai entered into a global license agreement granting Galderma S.A. of Switzerland exclusive rights for the development and marketing of nemolizumab worldwide, with the exception of Japan and Taiwan. In September 2016, Chugai entered into a license agreement granting Maruho Co., Ltd., the rights for the development and marketing of nemolizumab in the skin disease area for the Japanese market. In March 2022, Maruho received regulatory approval for nemolizumab in the treatment of itching associated with atopic dermatitis (only when existing treatment is insufficiently effective) in Japan. (Product name: Mitchga^®)
In-house (licensed out to 3^rd party)	small molecule Oral	orforglipron/LY3502970 Oral non-peptidic GLP-1 receptor agonist	Type 2 diabetes Obesity	Orforglipron is an oral non-peptidic GLP-1 receptor agonist created by Chugai. GLP-1 agonists have potent hypoglycemic action and induce weight loss, but convenience for patients has been an issue because they are conventionally administered in a subcutaneous injection. Because orforglipron is orally bioavailable, it is easier for patients to take, and is thus expected to contribute to the treatment of diabetes, including through improvement of drug adherence. In September 2018, Chugai licensed the worldwide development and commercialization rights for orforglipron to Eli Lilly and Company.
In-house	small molecule IV	REVN24 ―	Acute diseases	REVN24 is a small molecule drug developed in-house by Chugai.
Roche	RNAi SC	zilebesiran/RG6615 RNAi therapeutic targeting angiotensinogen	Hypertension	RG6615 is an investigational, subcutaneously administered RNAi therapeutic targeting angiotensinogen (AGT) in development for the treatment of hypertension in high unmet need populations. AGT is the most upstream precursor in the Renin-Angiotensin-Aldosterone System (RAAS), a cascade which has a demonstrated role in blood pressure regulation and its inhibition has well-established antihypertensive effects. RG6615 inhibits the synthesis of AGT in the liver, potentially leading to durable reductions in AGT protein and ultimately, in the vasoconstrictor angiotensin (Ang) II.

Response to Requests from the MHLW Review Committee on Unapproved Drugs and Indications with High Medical Needs (As of July 25, 2024)

Development Request	Product	Indication	Development Status
First development request	Xeloda	Advanced or recurrent gastric cancer	Approved in February 2011
	Tarceva	Advanced or recurrent pancreatic cancer	Approved in July 2011
	Avastin	Advanced or recurrent breast cancer	Approved in September 2011
	CellCept	Pediatric renal transplant	Approved in September 2011
	Herceptin	Q3W dosage metastatic breast cancer overexpressing HER2	Approved in November 2011
	Herceptin	Neoadjuvant breast cancer overexpressing HER2	Approved in November 2011
	Kytril	Gastrointestinal symptoms associated with radiotherapy	Approved in December 2011
	Pulmozyme	Improvement of pulmonary function in patients with cystic fibrosis	Approved in March 2012
	Bactramin	Treatment and prevention of pneumocystis pneumonia	Approved in August 2012
	Avastin	Ovarian cancer	Approved in November 2013
Second development request	Avastin	Recurrent glioblastoma	Approved in June 2013 (Malignant glioma)
	Herceptin	Q1W dosage postoperative adjuvant breast cancer overexpressing HER2	Approved in June 2013
	CellCept	Lupus nephritis	Approved in May 2016
Third development request	Tamiflu	Additional dosage for neonates and infants younger than 12 months	Approved in March 2017
	Xeloda	Adjuvant chemotherapy in rectal cancer	Approved in August 2016
	Avastin	Additional Q2W dosage and administration for ovarian cancer	Approved in June 2022
Fourth development request	Copegus	Improvement of viraemia associated with genotype 3 chronic hepatitis C or compensated cirrhosis related to hepatitis C when administered in combination with sofosbuvir	Approved in March 2017
	Xeloda	Neuroendocrine tumor	Submitted company opinion and waiting for evaluation by committee
	Avastin	Cerebral edema induced by radiation necrosis	Submitted company opinion and waiting for evaluation by committee
	Neutrogin	Combination therapy with chemotherapy including fludarabine for relapsed/refractory acute myeloid leukemia	Approved in June 2022
	CellCept	Prevention of graft-versus-host disease in hematopoietic stem cell transplantation	Approved in June 2021
	CellCept	Systemic sclerosis associated interstitial lung disease (SSc-ILD)	Approved in June 2024
	CellCept	Remission maintenance therapy following rituximab therapy for refractory nephrotic syndrome (frequently relapsing or steroid-dependent nephrotic syndrome)	Submitted company opinion and waiting for evaluation by committee

*Transferred the marketing authorization holder of Xeloda to CHEPLAPHARM K.K. as of February 1, 2024