|20/11/27||GEM232||Anti-soluble MICA/MICB antibody||Prostate Cancers （mCRPC）, other cancers||i.v.||Antibody
||Preclinical||- GEM232 is a humanized antibody specific for soluble NKG2D ligands MICA and MICB, which are multi-mechanistic suppressors of the immune system that become upregulated in cancer but are normally absent.
- GEM232 binds non-membrane bound MICA/B (shed/soluble forms) but not cell surface attached versions, thereby offering safety benefits such as avoiding autoimmunity.
- Antibody binding may help prevent immunosuppression and may enhance NK and CD8+ T cell activation mediated by the NKG2D receptor leading to tumor cell killing. Both arms of immune system (innate and adaptive) can be impacted.
- Significant tumor inhibition demonstrated using prostate xenografts in both immune compromised mice and in mice with humanized immune systems (hPBMC), with no observable toxicity. A unique epitope has been identified for this high affinity antibody.
|20/11/25||GEM231||JNK inhibitor||Dry Eye, Dry and Wet AMD, Uveitis, Chronic inflammation alternative to Steroids||Intra- vitreal, Subcon- junctival, Drops||Peptide
||Clinical Phase 3 （performed in acute post surgery）||・Potent and selective non-ATP competitive hJNK2 and hJNK3 inhibitor
・Full D amino acids – TAT peptide with high resistance to proteases and highly soluble in saline
・Coupled to a carrier sequence that selectively delivers it into the cell
・Excellent safety and toxicology profile (therapeutic indexes in 100 -1000 range)
・Administered to 1000+ patients to date with no sign of intolerance
・Excellent patent position
・Simple to manufacture at low COG per dose
|20/11/25||GEM230||Anti-CD38 scFv-Fc conjugation of lenalidomide||Multiple Myeloma||i.v.||Antibody-drug conjugates
- The conjugation does not affect cell binding affinity compared to parental antibodies.
- Conjugation with lenalidomide bundle did not affect ADCC/CDC activities on CD38+ cells
- In the multiple myeloma xenograft mouse model, TE-1146 has superior tumor suppression ability compared to parental antibody, Darzalex.
|20/11/25||GEM229||Insulin with fatty acids bundle||Type1/2 Diabetes||s.c.||Peptide conjugated fatty acid
- can be produced in high quality and activate AKT phosphorylation as degludec.
- can induce cell proliferation as degludec and inhibit cell apoptosis as degludec.
-can better reduce blood glucose than degludec and effectively control blood glucose level at lower dosage than degludec.
GEM229 shows better blood glucose control than degludec by once daily injection and better blood glucose control than degludec by every other day (Q2D) injection for 30 days.
GEM229 causes a significant reduction in HbA1C level after treating for 60 days
|20/11/25||GEM228||GLP-1 with fatty acids bundles||Type2 Diabetes, obesity; NASH||s.c.||Peptide conjugated fatty acid
-can be produced in high quality.
-can lower blood glucose better than semaglutide and effectively control blood glucose level at 10 nmol/kg
- can effectively reduce body weight and reduce liver fat
|20/11/25||GEM227||Octreotide with fatty acids bundles||carcinoid syndrome/ acromegaly||s.c.||Peptide conjugated fatty acid
- can be produced in high quality and bind to HSA effectively.
- Fatty acids bundle can effectively prolong serum half-life of octreotide and antiproliferative effect of GEM227 is similar to that of octreotide.
- can effectively reduce serotonin level in xenograft mouse model.
|20/11/25||GEM226||Anti-fibrin scFv with reteplase||Pathological Clots||i.v.||Antibody conjugated reteplase
- can bind to human fibrin/crosslinked fibrin, but not to fibrinogen and bind to human fibrin under high concentration of fibrinogen.
-GEM226 is stable in buffer at 4°C and alteplase showed similar enzyme kinetics to tPA substrate, also can dissolve clots effectively, accumulate at the clot in vivo and bind to human clots specifically
-GEM226 has better PK profile in rat and shows better clot-dissolving effect than that of alteplase in MCAO mice model.
-GEM226-treated MCAO stroke mice have better neurobehavior than the mice treated with alteplase
|20/11/24||GEM225||Regulating the cellular pathway that differentiates cancer cells, leading to apoptosis and cancer arrest||Triple negative breast cancer, Pancreatic cancer||i.v.||Protein
||Preclinical||- GEM225 is a recombinant human KL-1 (rhKL-1).
- KL-1 is the domain with the anti-cancer activity of Klotho, a hormone with tumor suppression activity.
- Klotho expression in epigenetically silenced in malignant tissues.
- rhKL-1 inhibited tumor growth in-vivo.
- rhKL-1 demonstrated acceptable safety profile in the in-vivo studies.
- rhKL-1 can provide effective and safe solution where currently approved treatments fail.
|20/11/02||GEM224||Pan-BET-Bromodomain inhibition||Inflammatory and fibrotic diseases. Acute lung injury induced by X-ray radiation or mechanical ventilation *（see note）||Oral||Small molecule||Preclinical （Non-GLP）||・Inhibit BET-bromodomain proteins BRD2, BRD3 and BRD4, but no other bromodomain proteins
・Against BRD4, as good or better compared to a reference compound but much simpler to synthesize (No chiral centers)
・Potential for inflammatory & fibrotic diseases
*Initial focused indication: prevention of acute lung injury induced by X-ray radiation (for breast or lung cancer) or mechanical ventilation (intensive care treatment)
・Supresses LPS-induced production of proinflamatory cytokines from whole human blood (in vitro) and ear edema (in vivo), and TGF-beta induced expression of collagen and Acta2 in liver stellate cells (in vitro)
・PK: oral bioavailability
・NCE, patent filed in 2019, allowed in US in 2020
|20/10/15||GEM223||Regulation of cellular phosphate handling and intracellular energy status||Hyperphospha-temia in chronic kidney disease （CKD） Chemotherapy-induced hyperphospha-temia （Tumor Lysis Syndrome, TLS）||Oral Intra-venous||Small molecule||Pre-IND||First-in-class drug with a new MOA that is completely different from those of existing drugs for the treatment of hyperphosphatemia in CKD and TLS, a serious complication in cancer patients.
- A unique and highly effective mechanism to reduce blood phosphate levels in mammals
- Once-daily dosing potential
- No gastrointestinal side-effects
- Mechanism-based kidney protective effects
- IND-enabling 4-week toxicological studies have been finished