Organic Active Ingredients TRIZ Cases

TCD compounds target the Sec61 translocon to block protein secretion with improved selectivity, manufacturability, and bio-availability.

Substituted pyrazinecarboxamides target EGFR del19/L858R T790M C797S mutants to address TKI resistance in non-small cell lung cancer.

Trisubstituted benzotriazole derivatives inhibit DHODH to expand treatment beyond autoimmune disease and suppress tumor growth and metastasis.

Adsorbed mutant NGF on biomaterial carriers speeds cartilage-to-bone healing while avoiding the pain and hyperalgesia seen with wild-type NGF.

Turbulent mixing of separate lipid and aminoglycoside streams enables scalable liposome production with high encapsulation efficiency and controlled particle size.

A room-temperature stable amlodipine oral liquid improves dosing accuracy and avoids tablet crushing hazards for children and elderly patients.

A benzotriazole-substituted compound improves ejaculation control with better efficacy than dapoxetine while aiming to reduce side effects.

Using SGLT-2 inhibition, enavogliflozin reduces nanoplastic-driven oxidative stress and protects endothelial function in cardiovascular aging disease.

Sub-anesthetic ketamine with NAP raises ADNP expression while limiting neurotoxicity, supporting treatment of ADNP syndrome and autism.

Targeting spike protein disulfide bonds with cysteamine helps prevent SARS-CoV-2 infection while limiting toxicity through controlled dosing.

Alumina adsorption and solvent precipitation tighten hydroxypropyl beta-cyclodextrin composition control for safer chronic intrathecal dosing.

Engineered vaccinia viruses disrupt B2R and add immune modulators to limit neutralization while preserving strong anti-tumor activity.

Crystalline OAD2 acid salts improve stability and hygroscopicity by changing the acid counterion while preserving GLP-1 agonist activity.

A viscous intranasal cannabidiol composition improves bioavailability by bypassing hepatic first-pass metabolism and supporting sustained brain delivery.

Oral JAK1 inhibition with upadacitinib improves response rates in axial spondyloarthritis, psoriatic arthritis, and psoriasis.

Selective mGlu2 negative allosteric modulators use tailored isoindolinone substituents to improve receptor specificity and therapeutic efficacy.

An alginate hydrogel forms a buoyant gastric implant after oral dosing and later dissolves by chelation, avoiding endoscopic placement and removal.

A high-ionic-strength oxymetazoline cream uses excipient and viscosity tuning to keep stability while reducing rosacea facial erythema.

Small-molecule GCS inhibitor derivatives reduce glucosylceramide buildup and target neurological limits of enzyme replacement therapy.

A branched linker and spacer layout gives trident aptamers stronger target binding while preserving orientation control and manufacturability.

Combining VS-6063 with CH5126766 targets FAK and RAS/RAF/MEK signaling to improve immune response in RAS-mutant ovarian cancer.

Sequential anti-FOLR1 combination therapy improves tumor response while maintaining or reducing toxicity in ovarian and related cancers.

Selective AhR-binding tetrahydro-β-carbolines raise IL-22 and inhibit IFN-γ to improve treatment of Crohn's and related inflammation.

A plant-based ALA-rich lipid blend uses single-source processing and antioxidants to limit oxidation and extend storage stability.

Formula (1) compounds in lipid particles raise nucleic acid encapsulation and delivery efficiency without the gene size limits of viral vectors.

An esterified lenalidomide derivative improves permeability and smooths plasma concentration peaks to reduce toxicity in multiple myeloma treatment.

An achiral tetrahydropyrimidinedione scaffold replaces chiral IMiD cores to preserve CRBN binding while lowering synthesis complexity.

Surfactant-based formulations inhibit perinucleolar compartments and nucleolar structure to curb pancreatic cancer metastasis with low toxicity.

Benzimidazole P-CAB derivatives improve neutral-water and pH-independent solubility while maintaining rapid gastric acid suppression.

Selected miRNAs activate dermal papilla cells and raise COL17A1 and VEGF expression to support hair regrowth and help prevent white hair.

Selective FGFR2/3 inhibition narrows off-target kinase activity to reduce hyperphosphatemia and diarrhea while treating FGFR-driven cancers.

Novel CRBN ligands use defined substituent changes to improve PROTAC selectivity while limiting unwanted domain protein degradation.

RNase III purification removes dsRNA from synthetic mRNA, reducing immune toxicity during repeated delivery for efficient iPSC reprogramming.

Stepwise linker-payload conjugation and stabilized anti-B7-H3 antibodies improve ADC homogeneity, targeting, and tumor inhibition with fewer side effects.

Selective pyrrolopyrimidine inhibition of FGFR2 and FGFR3 improves antitumor activity while avoiding FGFR1/4-linked side effects and resistance.

Topical lipoic acid controls myopia progression with more consistent effects across myopia types and fewer rebound concerns than existing drugs.

An acidic surfactant-based crisdesalazine formulation raises dissolution and bioavailability while limiting impurity growth during storage.

Pyridone compounds are tuned to inhibit Axl, Mer, KDR, and c-Met kinases, improving cancer treatment efficacy while addressing specificity limits.

Small molecules target PD-1/PD-L1 binding to restore T cell function while avoiding the cost and efficacy limits of antibody therapies.

Liposomal mitoxantrone combined with cytarabine helps address AML relapse while improving remission and survival with good tolerability.

Targeted joint cavity dosing uses a defined therapeutic regimen to prevent prosthetic joint infection recurrence and limit bacterial resistance.

Arginine stabilizes catechol cephalosporin formulations, avoiding ultra-low-temperature storage while preserving Gram-negative antibacterial activity.

A scored bilayer tablet separates tenofovir, emtricitabine, and efavirenz to improve stability, dissolution, hardness, and swallowing ease.

Locking gaps in a rectangular vaporizer cartridge base prevent user-induced movement and keep electrical contact stable during use.

Albumin-binding Evans Blue-PSMA conjugates extend blood half-life, raise tumor uptake, and improve prostate cancer imaging and radiotherapy.

Using pivaloyl chloride and a water/alkyl acetate biphasic system, this olaparib process improves yield and purity while reducing toxic solvent use.

A type I quinoline-substituted crystal uses controlled crystallization and PXRD-defined polymorph selection to improve stability and resist moisture.

Selective 15-PGDH compounds modulate prostaglandin levels while limiting broad dehydrogenase effects in disorders tied to prostaglandin regulation.

A water-free topical composition using diethylene glycol monoethyl ether and PEG 400 improves skin permeation, local retention, and formulation stability.

Capsaicin derivatives such as phenylcapsaicin inhibit PDGF-α/β to slow idiopathic pulmonary fibrosis with lower toxicity risk.

Biomarker-guided IL-6 receptor inhibition targets ocular inflammation while reducing treatment uncertainty and unnecessary exposure.

A PDE10 inhibitor offers tic reduction and neurobehavioral symptom control in Tourette syndrome without the significant side effects of neuroleptics.

Nitrogen-containing heterocyclic compounds inhibit SARS-CoV-2 and related coronaviruses while reducing host-cell cytotoxicity.

SAM-targeted aza-quinoline compounds inhibit EZH2 in PRC2, reactivate suppressed genes, and reduce tumor growth in EZH2-driven disease.

Novel substituent and ring modifications broaden JAK-STAT inhibition across inflammatory and neoplastic diseases while reducing toxicity.

Natural receptor-activating compounds induce endogenous GLP-1 and GIP secretion to treat obesity and type-2 diabetes without injections.

Homogenized MK-9 nanoparticles with emulsifier stabilization improve solubility and serum levels for treating vascular calcification and bone disease.

Separate vitamin and trace-element chambers keep ready-to-use parenteral nutrition stable through sterilization while avoiding manual additions.

Novel Carbonic Anhydrase 1 inhibitors improve mast cell and inflammation control with better potency and selectivity and fewer side effects.

Novel macrocyclic compounds inhibit KRAS, NRAS, and HRAS mutants in one agent, addressing resistance and limited utility of allele-specific therapies.

Prelinked neurotensin receptor ligands improve NTR1 tumor uptake and imaging while limiting brain exposure and affinity shifts from labeling.

Using HFO-1234ze(E), ethanol, and a sub-0.5 mm actuator orifice, this pMDI case balances low GWP with high fine particle delivery.

Intermittent JAK inhibitor dosing suppresses seizures after withdrawal and helps restore spatial memory in drug-resistant epilepsy.

Concurrent anti-PD-L1, optional anti-CTLA-4, and chemoradiation therapy improves response and survival in advanced solid tumors.

A protease cleavage switch lets engineered CAR receptors turn signaling on or off, reducing basal activity and limiting off-tumor adverse effects.

By degrading FAK instead of only inhibiting it, these compounds boost cytotoxic T-cell activity and reduce tumor immune resistance.

TERT inhibition before radiation or chemotherapy sensitizes resistant cancer cells, reduces immune evasion, and supports tumor elimination.

A dual-action amide compound targets 5-HT2A and 5-HT7 receptors in one molecule, simplifying treatment for neuropsychiatric diseases.

Solvent-free enteric beadlets keep capsaicinoid release below 10% in the stomach and enable rapid intestinal absorption with less gastric discomfort.

Dipeptoid-like cationic lipids add biodegradable ester bonds and modular coupling sites to improve RNA delivery, targeting, and serum protection.

Small-molecule indolinones block EWS-FLI1 and RNA helicase A binding, avoiding antisense and siRNA delivery and stability limits.

Stable hydrochloride and succinate salt forms of the S-enantiomer improve ROCK inhibitor stability and reduce off-target kinase inhibition.

A non-aqueous pantoprazole formulation uses polyethylene glycol and pH stabilization to enable room-temperature storage and direct injection.

When standard ILD drugs show limited benefit, treprostinil helps improve pulmonary function and increase forced vital capacity.

Combining MTDP and PLK1 inhibitors helps suppress cancer progression and address resistance through coordinated dosing.

Polycyclic quinazolines improve ERBB2 selectivity over EGFR, helping treat Exon 20 mutant cancers with lower toxicity.

Biocompatible polymers repair pulmonary tissue, restore respiratory function, and protect the alveolar-capillary barrier in microbial lung lesions.

A cyclic oligonucleotide masks the 5′ end to reduce PRR-triggered inflammation while improving nuclease stability and target RNA activity.

Using NMN as an NAD precursor in child nutrition helps improve exercise capacity while reducing triglycerides, glucose, and fat accumulation.

A controlled-release exendin-4 or exenatide formulation uses polymer and basic amino acid coating to cross the blood-brain barrier and curb dyskinesia.

Controlled H/C-ratio polyoxazoline nanoaggregates encapsulate poorly soluble bioactive agents to improve solubility, delivery, and scalable formulation.

Chemically modified dsRNA targets hepatocytes via asialoglycoprotein receptors to silence APOC3 and lower triglycerides.

A two-component PEG hydrogel uses pH-controlled rapid setting to seal deflated lungs with lower stiffness, stronger adhesion, and better coverage.

A T4 capsid with lipid coating and sequential payload assembly enables safer, high-efficiency delivery of DNA, RNA, and Cas9 into human cells.

Novel tetrahydro-pyridoindole ER modulators address metastatic and acquired resistance while treating estrogen receptor-mediated cancers.

β-cyclodextrin boosts bilastine solubility for IV or IM dosing, enabling rapid 15-minute action and 24-hour relief without sedation.

A reservoir and outlet route drugs through a tympanostomy tube to the middle ear while maintaining pressure equalization and controlled release.

Specific salt and crystal forms improve 15-PGDH inhibitor druggability and stability through XRPD, DSC, and TGA characterization.

Novel SIK1/2/3 inhibitor compounds rebalance cytokines by lowering TNFα and IL-12 while raising IL-10 for inflammatory and autoimmune disease treatment.

Structural tuning of piperazinyl norbenzomorphan compounds improves sigma 2 receptor subtype selectivity while preserving receptor modulation.

Plant-derived sterols restore aged asphalt binder processability and slow oxidation, enabling higher RAP and RAS reuse in pavement production.

DVAP-modified exosomes co-deliver mitoxantrone and siNotch1 to target residual glioma initiating cells and help limit recurrence.

Deuterium substitution in camptothecin improves in vivo stability and lowers toxicity while preserving tumor treatment activity.

A modular FAP-targeting ligand with an integrated chelator improves radiolabeling, stability, and tumor-to-organ biodistribution.

Cinnamic acid is used to relieve chemotherapy-induced allodynia while minimizing side effects and preserving anticancer activity.

A single compound inhibits RIPK2, c-abl, and LRRK2 to reduce inflammation and neurodegeneration across related diseases.

Specific absorbent and crystallization-inhibitor ratios help skin adhesives deliver drugs with more predictable release and extended compatibility.

Glutamate raises saliva pH through decarboxylation to GABA, helping rebalance oral microbiota and reduce caries risk.

HTLV-1 Gag p15, p19, and p24 antigens are used to trigger immune response and help prevent ATL onset or relapse after transplantation.

Direct subungual delivery of liquid antifungal via a blunt-tip cannula reaches the nail bed while avoiding trauma and systemic toxicity.

Linker-based riluzole prodrugs bypass rapid hepatic metabolism after oral dosing and release riluzole in plasma for steadier exposure.

Controlled granule size and excipient ratios let a daprodustat dispersible tablet break down in 1-5 mL water into a free-flowing, palatable suspension.

Dose escalation from 160 mg to 200-300 mg/day offsets CYP3A4 inducer metabolism and helps maintain anticancer drug efficacy.

Small quinoline antagonists inhibit aberrant cGAS activation to curb autoimmune and inflammatory signaling while preserving therapeutic utility.

DMSO and glycofurol retard melatonin breakdown in aqueous topical solutions, preserving stability and bioactivity during storage.

LONRF2 uses conformational binding and ubiquitination to detect and reduce structurally abnormal proteins linked to mammalian neurodegeneration.

Surfactant-based liquid extraction dissolves or emulsifies cannabinoids and terpenes, enabling simpler purification without high-pressure CO2 or wax-heavy ethanol steps.

Alternating electric fields temporarily open the blood-brain barrier for large drug delivery, then allow recovery for repeated treatment cycles.

A selective norepinephrine inhibitor approach uses reboxetine to reduce cataplexy attacks, ease sleepiness, and avoid DEA scheduling limits.

Gene-edited donor animals suppress immune-triggering genes to create transplantable organs with lower rejection risk and less need for chronic immunosuppression.

By inhibiting CYP2D6 metabolism, bupropion raises dextromethorphan exposure to improve depression response and reduce suicidal ideation.

DHMBA suppresses inflammatory macrophage proliferation, cytokine production, and osteoclast formation to support treatment of inflammatory diseases.

Small-molecule CD73 inhibitors block AMP hydrolysis to limit adenosine-driven immune suppression and improve treatment response.

Lipid-core nanoparticles localize innate immune activation to deliver higher RNA doses while reducing systemic inflammation and reactogenicity.

Small-molecule receptor modulators improve glucose metabolism and weight loss while simplifying treatment of calcitonin- and amylin-linked disorders.

Targeted BTK inhibition reduces mast cell activation in indolent systemic mastocytosis, improving symptom control with minimal adverse effects.

Pulmonary delivery of TSLP-targeting RNAi agents enables selective gene silencing in airway cells while reducing injection burden in asthma treatment.

A 2-methoxyestradiol and Chir99021 combination reduces collagen deposition and tissue damage in radiation-induced lung fibrosis.

Local anti-Semaphorin 4D antibody injection blocks immune cell infiltration in salivary glands to treat hyposalivation with fewer systemic side effects.

Combining estetrol with drospirenone reduces unscheduled bleeding and spotting in adolescents while maintaining contraceptive efficacy.

Amaranth flour absorbs and stabilizes volatile mint oil extract in powder form, improving bioavailability and LDL cholesterol reduction.

Asymmetric catalytic cyclization replaces reagent-heavy routes to gamma-carbolines, improving yield, enantiomeric purity, and cleanup.

Single-stranded AONs recruit endogenous ADAR to edit a chosen adenosine in target RNA without recombinant enzymes, improving specificity.

Microencapsulated glutathione and milk thistle extract improve oral mucosal absorption, stability, and liver-support efficacy in films and stick jelly.

Multiple FXR agonist polymorphs improve formulation flexibility and stability while supporting efficacy in metabolic, liver, and inflammatory disorders.

By targeting CD13 with TNF or IFN chimeric proteins, this case shows localized immune recruitment and tumor vasculature disruption with lower toxicity.

Reporter-guided flow cytometry enriches aptamers by cellular function, not binding alone, improving selection of therapeutic candidates.

Liposome and nanoparticle delivery of DLPC or DPPC improves solubility and liver targeting to reduce fibrosis and inflammation.

Multi-thiol polyglycerol derivatives penetrate mucus gels and break disulfide bridges to lower viscosity in CF, COPD, and related disorders.

Combining ALK and CDK inhibitors improves NSCLC treatment response, helps overcome resistance, and supports safer dosing schedules.

Enzyme-cleavable linkers and self-immolative spacers help TROP2 ADCs release cytotoxins more selectively, improving tumor killing and safety.

Using L-BAIBA or D-BAIBA instead of racemic BAIBA improves metabolic markers, lowers body fat and glucose, and works even without exercise.

Circular polyribonucleotides use embedded regulatory elements to boost translation, extend half-life, and lower immunogenicity in cells.

Stable maribavir polymorphs and dosing strategies limit in vivo isomerization, improving bioavailability and antiviral efficacy.

By recruiting target proteins to E2 enzymes instead of E3 ligases, these PROTAC compositions reduce mutation-driven resistance while enabling degradation.

Targeting GlyT1 inhibits heme and red blood cell synthesis to lower hemoglobin, reduce complications, and limit phlebotomy needs.

An absorbent wipe balances pramoxine, diphenhydramine, and soothing agents to treat pet skin conditions without irritating ears, eyes, or nose.

Novel isothiazolyl and isoxazolyl sulfonamides modulate GPR17 to drive OPC differentiation and improve CNS myelination and remyelination.

Selective alpha-biased IL-2 helps stabilize kidney transplants and reduce rejection while avoiding broad immunosuppression risks.

Localized magnetic heating and free radicals boost tumor immunogenicity, helping checkpoint blockade suppress relapse and metastasis.

A PICVD multilayer syringe coating adds smoothing, barrier, and protection layers to limit air diffusion, reduce leachables, and resist pH stress.

Oral dosing of an optically active azabicyclo menin inhibitor improves treatment of MLL-rearranged leukemia while balancing efficacy and safety.

An alkaline aqueous pH 10.5 formulation keeps gemfibrozil soluble and stable in oral liquid form while avoiding complex solvent systems.

A camptothecin-based ADC toxin molecule improves tumor cell inhibition while reducing toxicity to normal cells through targeted antibody delivery.

Ionizable lipid nanoparticles improve nucleic acid transfection while lowering toxicity and avoiding viral insertional mutagenesis.

CBDA ester compounds improve cannabinoid stability while expanding therapeutic use across inflammatory, gastrointestinal, uterine, and metabolic disorders.

A six-ingredient milk thistle formula targets alcohol-related liver damage and multiple liver conditions through combined antioxidant and protective effects.

Base modifications such as m5C, ψ, and m1ψ help RNA nanostructures evade innate immune sensing while preserving shape and stability.

A BTK inhibitor composition treats MOGAD by reducing relapses and antibody titers while lowering liver injury risk.

Chemical substitutions create selective AT2 agonists with better metabolic stability and lower CYP inhibition for interstitial lung disease treatment.