Weight loss can also easily "lie to win"? In the analysis of weight loss therapy in research, three positive trends were glimpsed

In 2022, the hottest summer in history, burning calories has become an urgent need

Weight loss of up to 22.

Based on the huge unfinished needs in the field of weight loss, WuXi AppTec content team has compiled the latest clinically developed drug pipeline for the indication of weight loss (as of August 3, 2022)

According to incomplete statistics, there are currently 31 research slimming therapies

Content Summary of 31 researched weight loss therapies

Drug development trend one: target diversification

Drug development trend one: target diversification

Incretin therapy, represented by GLP-1 receptor agonists, dominates

GLP-1 receptor agonist

The therapeutic targets in the phase 2 clinical development stage are more abundant and the mechanisms are more novel, including controllable metabolic accelerators, neuropeptide YY5 receptors, IKKε/TBK1, activator type II receptors, etc.

The variety of therapeutic targets in the Phase 2 clinical development phase is more abundant

Drug development trend two: the future will vigorously develop oral dosage forms

Drug development trend two: the future will vigorously develop oral dosage forms

The number of oral and injectable drugs is roughly the same, and the proportion of oral dosage forms decreases with the decrease in the state of development, but the proportion in phase 2 clinical phases has rebounded to 53%.

The number of oral and injectable drugs is roughly equivalent

Drug development trend three: weight loss effect breaks through the bottleneck

Drug development trend three: weight loss effect breaks through the bottleneck

From the marketing, pre-registration to the phase 3 clinical stage, the weight reduction effect of the drug has been steadily improved, and the previous 5%-10% weight reduction bottleneck

The weight loss effect of the drug has steadily increased by 5%-10% of the weight loss bottleneck

Target: GLP-1 receptor-dominant, multiple mechanisms of incretin insulin growth at high speed

Target: GLP-1 receptor-dominant, multiple mechanisms of incretin insulin growth at high speed

In each stage of development, from Phase 2 clinical to marketing, the number of therapies targeting GLP-1 receptors is the largest

The therapies targeting the GLP-1 receptor are the largest number of approved marketers of GLP-1 receptor agonists

Specifically, GLP-1 receptor agonists account for 30% of listed drugs, 50% of pre-registered drugs, and 18% of Phase 2 drugs, which shows that the proportion of single GLP-1 receptor agonists in early clinical development therapies has gradually decreased, while double and triple receptor agonists such as GLP-1/GCG,GLP-1/GIP, GLP-1/GCG/GIP are more distributed in Phase 2 and Phase 3 clinical trials, but have not yet entered the pre-registration and marketing stages.

The proportion of single GLP-1 receptor agonists in early clinical development of therapies gradually decreases

In addition to the targets of enterointropic insulin, from the market to the phase 2 stage, the therapy has generally shown a trend

The therapy generally shows a trend of increasingly diversified and novel targets

In addition to the GLP-1 receptor agonists, tesofensine is still an SNDRIs in the 2 pre-registered therapies

Finally, in 17 therapies for Phase 2 clinical trials, there are 8 non-enteric insulin-stimulating mechanisms, namely controllable metabolic accelerators (CMAs), neuropeptide YY5 receptors, appetite-regulating hormones, important regulators of metabolic diseases IKKε/TBK1, SIRT1 protein, activator type II receptors, bitter taste receptor TAS2R, amylase/glucosidase, these mechanisms are relatively novel

In phase 2 clinical trials, there are 8 non-enteric insulin mechanisms of action that can be limitedly activated by the mitochondrial decompolytic industry, and the industry is actively exploring innovative strategies for the treatment of weight loss

Dosage form: slightly more oral than injectable, the future development trend of oral dosage form is better

Dosage form: slightly more oral than injectable, the future development trend of oral dosage form is better

Of the 31 drugs, 16 are oral and 15 are injectable

Due to the increase in the proportion of enterointropic insulin therapy, the proportion of oral drugs has decreased, and the trend of oral weight loss therapy may be better than injection

Weight loss effect: "Latecomers" are on top, and the upper limit is constantly increasing

Weight loss effect: "Latecomers" are on top, and the upper limit is constantly increasing

▲The effect of different weight loss therapies on weight reduction (Image source: Reference[1])

▲The effect of different weight loss therapies on weight reduction (Image source: Reference[1])

The effect of weight loss therapy is a topic of great concern, here is cited in nature Reviews Drug Discovery's weight loss therapy review data, in the existing weight loss methods, the effect of bariatric surgery is the most significant, the average weight loss of up to about 30%, but the implementation of bariatric surgery for patients has more stringent conditions, and surgical risk, postoperative recovery is also an uncertain factor

The most significant effect of bariatric surgery Weight loss drugs greatly surpass surgical surgery in terms of convenience and safety, but the weight loss effect is not as good as the former

So whether weight loss drugs have made progress in weight loss effect since entering 2022, we have conducted some simple analysis

The results showed that the average weight loss percentage of marketed, pre-registered, and phase 3 weight loss drugs increased sequentially, and the upper limit of the weight loss effect of drugs was constantly increasing

The average weight loss percentage of marketed, pre-registered, and phase 3 weight loss drugs has increased sequentially, and the upper limit of the weight loss effect of drugs is constantly increasing

Although the current drug in the public perception is not the preferred method of weight loss, most of the weight loss drugs are still in the early stage of development, but the three major trends of target diversification, dosage form convenience improvement, weight loss effect improvement reflect the industry's attention and investment in weight loss therapy, and look forward to more effective, safe and convenient weight loss drugs can appear as soon as possible to alleviate the expanding public health crisis
of the global obese population.